Biased Signaling Atlas

Ligand source activities (1 row/activity)

Potency
Affinity

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	AssayType	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	1324	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	16154396	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	16197727	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	44285019	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	57514683	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	91898441	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	CHEMBL441738	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	DB04931	7090	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	CHEMBL413212	219834	0	None	3	4	Human	10.7	pEC50	=	10.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	CHEMBL428615	220239	0	None	1	5	Human	10.7	pEC50	=	10.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	1324	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	16154396	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	16197727	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	44285019	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	57514683	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	91898441	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	CHEMBL441738	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	DB04931	7090	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	155527254	178029	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4460053	178029	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
	57646411	83696	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070245	83696	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	1323	9465	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	92432	9465	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL430239	9465	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	1323	9465	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	92432	9465	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	CHEMBL430239	9465	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	118722941	123020	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358549	123020	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722937	123016	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358545	123016	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722933	123013	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358541	123013	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	1323	9465	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	92432	9465	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	CHEMBL430239	9465	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	155551846	181913	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
	CHEMBL4569789	181913	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
	CHEMBL415661	219977	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL2371851	216918	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0490843
	118722944	123023	0	None	1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358552	123023	0	None	1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	1323	9465	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	92432	9465	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	CHEMBL430239	9465	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	44310104	88363	0	None	-4	4	Mouse	10.1	pEC50	=	10.1	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1040	16	13	13	-1.5	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303608
	CHEMBL216295	88363	0	None	-4	4	Mouse	10.1	pEC50	=	10.1	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1040	16	13	13	-1.5	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303608
	1324	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	16154396	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	16197727	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	44285019	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	57514683	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	91898441	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	CHEMBL441738	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	DB04931	7090	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	118722930	123011	0	None	-1	4	Mouse	10.0	pEC50	=	10.0	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358539	123011	0	None	-1	4	Mouse	10.0	pEC50	=	10.0	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL412495	219777	0	None	-	1	Human	10.0	pEC50	=	10	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	16746823	24929	0	None	-	1	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269576	24929	0	None	-	1	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL2372570	217050	0	None	-1	4	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O	10.1021/jm9017866
	CHEMBL407809	219464	0	None	-	1	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643803	118520	0	None	-3	5	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-3	5	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	10408	7507	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	5329	7507	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	9941379	7507	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	CHEMBL2070241	7507	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	DB11653	7507	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	1323	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	92432	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	CHEMBL430239	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	1323	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	92432	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	CHEMBL430239	9465	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	118722926	123008	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358535	123008	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	1324	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16154396	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16197727	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	44285019	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	57514683	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	91898441	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL441738	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	DB04931	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	1324	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	16154396	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	16197727	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	44285019	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	57514683	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	91898441	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	DB04931	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL5090946	222064	0	None	-4	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	118722931	123012	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358540	123012	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	118722938	123017	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358546	123017	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722942	123021	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358550	123021	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722943	123022	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358551	123022	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	1324	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	16154396	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	16197727	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	44285019	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	57514683	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	91898441	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	CHEMBL441738	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	DB04931	7090	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	127036484	143223	0	None	-2	4	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735690	143223	0	None	-2	4	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	1324	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	16154396	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	16197727	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	44285019	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	57514683	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	91898441	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	DB04931	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	1324	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	16154396	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	16197727	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	44285019	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	57514683	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	91898441	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	DB04931	7090	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	57646437	83697	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684621	83697	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929804	83697	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070246	83697	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	127036484	143223	0	None	-2	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735690	143223	0	None	-2	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL266879	217485	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0501432
	57646441	83695	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070243	83695	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL1688107	215613	0	None	1	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL5083551	221648	0	None	-10	4	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL2369484	216406	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL3646885	218802	0	None	74	2	Human	9.7	pEC50	=	9.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	118722927	123009	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358536	123009	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3287329	218090	0	None	1	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	16154396	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	16197727	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	44285019	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	57514683	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	91898441	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	DB04931	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	44415914	146048	0	None	5	3	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL379054	146048	0	None	5	3	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	10408	7507	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	5329	7507	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	9941379	7507	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	CHEMBL2070241	7507	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	DB11653	7507	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	1324	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	16154396	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	16197727	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	44285019	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	57514683	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	91898441	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	DB04931	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	1324	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	16154396	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	16197727	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	44285019	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	57514683	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	91898441	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	DB04931	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	1324	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16154396	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16197727	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	44285019	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	57514683	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	91898441	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL441738	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	DB04931	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL405087	219320	0	None	-1	5	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	1324	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16154396	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16197727	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	44285019	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	57514683	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	91898441	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL441738	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	DB04931	7090	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL2372859	217079	1	None	2	3	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/jm501027w
	90643808	118524	0	None	-14	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	16154396	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	16197727	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	44285019	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	57514683	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	91898441	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	DB04931	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	1324	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16154396	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16197727	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	44285019	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	57514683	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	91898441	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	DB04931	7090	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16132144	216058	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	16133793	216058	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	44273719	216058	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	CHEMBL214332	216058	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	CHEMBL5080489	221468	0	None	1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	118722936	123015	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358544	123015	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	50899078	24926	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269573	24926	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL2373515	217158	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643802	118519	0	None	-14	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3646890	218807	0	None	72	2	Human	9.6	pEC50	=	9.6	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	10408	7507	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	5329	7507	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	9941379	7507	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	CHEMBL2070241	7507	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	DB11653	7507	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	56659456	70475	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801215	70475	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL408257	219483	0	None	2	2	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643804	118521	0	None	-8	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL264352	217396	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL1688107	215613	0	None	1	4	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL5087839	221899	0	None	2	3	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1324	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	16154396	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	16197727	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	44285019	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	57514683	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	91898441	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	DB04931	7090	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	CHEMBL267900	217516	0	None	5	2	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL491870	220856	0	None	-9	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	118722932	122296	0	None	-1	4	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3352878	122296	0	None	-1	4	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	90643805	118522	0	None	1	5	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	1	5	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	16154396	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	16197727	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	44285019	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	57514683	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	91898441	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	DB04931	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	118735099	125577	0	None	4	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421676	125577	0	None	4	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	118735101	125579	0	None	9	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421678	125579	0	None	9	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	44415913	86726	0	None	-4	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL212614	86726	0	None	-4	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL385556	219133	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL3037885	217705	0	None	-1	2	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	16154396	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	16197727	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	44285019	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	57514683	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	91898441	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	DB04931	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	CHEMBL3646880	218798	0	None	29	2	Human	9.5	pEC50	=	9.5	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	CHEMBL5090285	222032	0	None	-1	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL3358542	218348	0	None	2	3	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(C)=O)C(N)=O	10.1021/jm501027w
	1324	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	16154396	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	16197727	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	44285019	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	57514683	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	91898441	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	DB04931	7090	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	CHEMBL429236	220295	0	None	-15	4	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	44416057	87966	0	None	1	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215833	87966	0	None	1	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	137637283	162759	0	None	2	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins	ChEMBL	984	15	12	10	-0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4061566	162759	0	None	2	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins	ChEMBL	984	15	12	10	-0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	122194229	130761	0	None	-14	5	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	CHEMBL3629347	130761	0	None	-14	5	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	1323	9465	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	92432	9465	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	CHEMBL430239	9465	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	CHEMBL415165	219955	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	56666386	70476	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801216	70476	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
	56676638	70467	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801146	70467	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL414965	219945	0	None	-8	5	Mouse	9.4	pEC50	=	9.4	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	11993702	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	5416	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	9272	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	CHEMBL3301624	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	DB11700	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	1324	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	16154396	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	16197727	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	44285019	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	57514683	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	91898441	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	DB04931	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	11993702	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	5416	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	9272	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	CHEMBL3301624	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	DB11700	10365	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	1324	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16154396	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16197727	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	44285019	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	57514683	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	91898441	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL441738	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	DB04931	7090	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL491870	220856	0	None	3	5	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	90643806	118523	0	None	-12	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	16154396	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	16197727	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	44285019	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	57514683	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	91898441	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	DB04931	7090	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	CHEMBL3646891	218808	0	None	30	2	Human	9.4	pEC50	=	9.4	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	16172929	219780	15	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL412536	219780	15	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	6918780	70241	1	None	204	2	Human	9.4	pEC50	=	9.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL179836	70241	1	None	204	2	Human	9.4	pEC50	=	9.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL386081	219154	0	None	-23	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O	10.1021/jm010061n
	CHEMBL444219	220709	0	None	4	4	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	CHEMBL3287327	218089	0	None	-5	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL267794	217512	0	None	-13	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL405335	219335	0	None	-2	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	CHEMBL5090670	222056	0	None	3	4	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1324	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	16154396	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	16197727	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	44285019	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	57514683	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	91898441	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	DB04931	7090	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	CHEMBL2070244	215963	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	122194229	130761	0	None	-14	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.10.095
	CHEMBL3629347	130761	0	None	-14	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.10.095
	44416106	148224	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL384176	148224	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44448629	174242	0	None	3	4	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL429854	174242	0	None	3	4	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL3646882	218800	0	None	35	2	Human	9.3	pEC50	=	9.3	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	1324	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL413912	219879	0	None	-7	3	Human	9.3	pEC50	=	9.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.07.046
	1324	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	16154396	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	16197727	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	44285019	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	57514683	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	91898441	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	CHEMBL441738	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	DB04931	7090	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	CHEMBL5080784	221485	0	None	-2	4	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL264132	217385	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cncn2C)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	45487403	204214	0	None	-53	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	788	22	9	7	2.4	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569693	204214	0	None	-53	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	788	22	9	7	2.4	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL414718	219930	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
	127047475	146527	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	132991507	146527	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798421	146527	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL428801	220251	0	None	-21	5	Human	9.2	pEC50	=	9.2	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	118722939	123018	0	None	1	4	Mouse	9.2	pEC50	=	9.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358547	123018	0	None	1	4	Mouse	9.2	pEC50	=	9.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	10146211	71103	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL181162	71103	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	56669819	70465	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801144	70465	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
	49862748	21921	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209799	21921	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
	1323	9465	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	92432	9465	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	CHEMBL430239	9465	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	10146211	71103	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL181162	71103	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	11061068	38066	0	None	138	3	Human	9.2	pEC50	=	9.2	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
	CHEMBL140154	38066	0	None	138	3	Human	9.2	pEC50	=	9.2	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
	1338	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL3646884	218801	0	None	39	2	Human	9.2	pEC50	=	9.2	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	CHEMBL412523	219779	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	129627786	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	1330	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16129617	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16129674	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133751	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133802	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16162116	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	3767	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	4516	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	60210072	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	6965	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL2103784	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	DB01284	7068	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16132144	216058	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	16133793	216058	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	44273719	216058	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	CHEMBL214332	216058	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	127046235	146416	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3797690	146416	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL428326	220217	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
	CHEMBL406842	219403	0	None	-6	5	Mouse	9.2	pEC50	=	9.2	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	56662904	70477	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801217	70477	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	90643803	118520	0	None	-1	5	Mouse	9.2	pEC50	=	9.2	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-1	5	Mouse	9.2	pEC50	=	9.2	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1338	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	1324	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	16154396	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	16197727	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	44285019	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	57514683	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	91898441	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	CHEMBL441738	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	DB04931	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	1324	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	16154396	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	16197727	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	44285019	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	57514683	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	91898441	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	CHEMBL441738	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	DB04931	7090	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	56669820	70468	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
	CHEMBL1801147	70468	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
	CHEMBL410763	219617	0	None	-21	4	Mouse	9.1	pEC50	=	9.1	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL412494	219776	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL3601426	218605	0	None	17	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	56676632	70452	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801118	70452	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	25129453	178545	0	None	15	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
	CHEMBL446757	178545	0	None	15	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
	49862750	21924	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209801	21924	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL3358537	218347	0	None	-3	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	1338	10579	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL3646889	218806	0	None	31	2	Human	9.1	pEC50	=	9.1	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	118722940	123019	0	None	-1	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358548	123019	0	None	-1	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3646892	218809	0	None	25	2	Human	9.1	pEC50	=	9.1	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	56673302	70445	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801095	70445	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	1324	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16154396	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16197727	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	44285019	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	57514683	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	91898441	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	DB04931	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL5077095	221258	0	None	-25	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16746686	24928	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269575	24928	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	25133210	176236	0	None	44	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
	CHEMBL442829	176236	0	None	44	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
	25131478	176287	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
	CHEMBL443396	176287	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
	44569176	179324	0	None	48	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
	CHEMBL448410	179324	0	None	48	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
	44275650	100829	0	None	-2	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	953	15	12	10	-0.8	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL24892	100829	0	None	-2	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	953	15	12	10	-0.8	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	16154396	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	16197727	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	44285019	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	57514683	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	91898441	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	DB04931	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	1324	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	16154396	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	16197727	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	44285019	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	57514683	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	91898441	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	DB04931	7090	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	10886436	125935	0	None	-1	5	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/acs.jmedchem.0c02041
	CHEMBL342954	125935	0	None	-1	5	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/acs.jmedchem.0c02041
	44448660	101748	0	None	4	4	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254589	101748	0	None	4	4	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	56659466	70447	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801097	70447	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL427666	220143	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O	10.1021/jm0501432
	CHEMBL264190	217387	1	None	-30	8	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL264536	217406	5	None	-20	4	Mouse	9.0	pEC50	=	9.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm010061n
	127048118	179786	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4518266	179786	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL5087859	221902	0	None	-4	3	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	56683301	70471	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801150	70471	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
	1324	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	16154396	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	16197727	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	44285019	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	57514683	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	91898441	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	CHEMBL441738	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	DB04931	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	1338	10579	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	9938402	10579	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	CHEMBL339053	10579	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	56679968	70469	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801148	70469	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
	70688853	83699	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070248	83699	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	1324	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	11571540	141987	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372201	141987	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11593230	168009	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1	10.1016/j.bmcl.2005.08.083
	CHEMBL411817	168009	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1	10.1016/j.bmcl.2005.08.083
	1324	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	16154396	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	16197727	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	44285019	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	57514683	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	91898441	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	CHEMBL441738	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	DB04931	7090	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	11851038	147113	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL5076315	221207	0	None	-3	4	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL3287059	218077	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL502093	220928	0	None	2	3	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	CHEMBL3799094	219047	0	None	-8	5	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56673305	70457	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
	CHEMBL1801123	70457	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
	56676639	70470	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801149	70470	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
	49862736	21909	0	None	117	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209787	21909	0	None	117	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	1324	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	16154396	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	16197727	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	44285019	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	57514683	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	91898441	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	CHEMBL441738	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	DB04931	7090	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	46919520	21910	0	None	2	6	Rat	9.0	pEC50	=	9.0	Functional	Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	21910	0	None	2	6	Rat	9.0	pEC50	=	9.0	Functional	Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	1324	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1324	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	168281421	197736	0	None	-10	3	Human	9.0	pEC50	=	9.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5185945	197736	0	None	-10	3	Human	9.0	pEC50	=	9.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	11158573	77894	0	None	-2	4	Mouse	8.9	pEC50	=	8.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	783	25	9	7	2.1	CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL195439	77894	0	None	-2	4	Mouse	8.9	pEC50	=	8.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	783	25	9	7	2.1	CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	127047853	146771	0	None	-4	5	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799955	146771	0	None	-4	5	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56676614	70478	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801218	70478	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	25129107	180556	0	None	36	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
	CHEMBL453734	180556	0	None	36	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
	1324	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1338	10579	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL5077144	221264	0	None	-13	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5090946	222064	0	None	-4	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL322610	218013	0	None	-2	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL5091236	222078	0	None	-48	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44408287	82161	0	None	162	4	Human	8.9	pEC50	=	8.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL203911	82161	0	None	162	4	Human	8.9	pEC50	=	8.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	56659467	70460	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
	CHEMBL1801126	70460	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
	25133556	195628	0	None	7	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
	CHEMBL506762	195628	0	None	7	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
	168276507	197044	0	None	-15	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5175487	197044	0	None	-15	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	168289457	198159	0	None	-7	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5192329	198159	0	None	-7	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137638778	163537	0	None	11	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4070639	163537	0	None	11	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	137633806	163260	0	None	10	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	CHEMBL4067491	163260	0	None	10	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	56662925	70450	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801116	70450	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL503229	220942	0	None	-1	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
	134466953	163437	0	None	-4	4	Mouse	8.9	pEC50	=	8.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1153	14	13	12	-1.3	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4069451	163437	0	None	-4	4	Mouse	8.9	pEC50	=	8.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1153	14	13	12	-1.3	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	1324	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44310344	104104	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	77231883	104104	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL269274	104104	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL443071	220699	0	None	-1	4	Human	8.9	pEC50	=	8.9	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	CHEMBL410404	219598	0	None	-11	5	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	10408	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	5329	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	9941379	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	CHEMBL2070241	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	DB11653	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	10408	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	5329	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	9941379	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	CHEMBL2070241	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	DB11653	7507	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	1338	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	9938402	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL339053	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL3358533	218346	0	None	-3	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	49862745	21918	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
	CHEMBL1209796	21918	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
	90643803	118520	0	None	-3	5	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-3	5	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1338	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL5087814	221898	0	None	-4	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16132144	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	16133793	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	44273719	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	44415920	87146	0	None	2	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL214410	87146	0	None	2	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44416060	88093	0	None	66	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215895	88093	0	None	66	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44415912	146004	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL378837	146004	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	56683299	70463	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801142	70463	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	134463477	166031	0	None	-5	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	977	11	12	11	-1.9	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4099127	166031	0	None	-5	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	977	11	12	11	-1.9	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	101670969	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	16131138	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	44349184	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	53310908	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	91898438	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	CHEMBL438402	175675	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	118722935	123014	0	None	1	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358543	123014	0	None	1	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	42630327	162650	0	None	-6	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
	CHEMBL4060381	162650	0	None	-6	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
	16007263	86571	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL211975	86571	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	56683300	70464	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801143	70464	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	25129109	195481	0	None	29	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
	CHEMBL504349	195481	0	None	29	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
	16132144	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	16133793	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	44273719	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	168293710	198945	0	None	-19	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5203986	198945	0	None	-19	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	168289404	198091	0	None	-39	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5191309	198091	0	None	-39	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137635422	162689	0	None	30	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060816	162689	0	None	30	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL264190	217387	1	None	-30	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	24848934	85727	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113004	85727	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
	16132144	216058	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	16133793	216058	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	44273719	216058	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	155531854	178427	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2286	54	25	25	-4.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4466007	178427	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2286	54	25	25	-4.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	155563057	182077	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4573190	182077	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56662927	70462	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
	CHEMBL1801141	70462	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
	CHEMBL3287069	218086	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)c(I)c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	44456222	104701	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272538	104701	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	49862376	21812	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209319	21812	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	25133208	178773	0	None	4	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
	CHEMBL447117	178773	0	None	4	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
	145977650	170613	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4206406	170613	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	1323	9465	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	92432	9465	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL430239	9465	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	11845272	87133	0	None	9	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL214347	87133	0	None	9	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	44275265	168069	0	None	14	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL412174	168069	0	None	14	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	90643802	118519	0	None	-14	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	218089	0	None	-5	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	11851038	147113	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44409257	147364	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	CHEMBL381357	147364	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	44409338	175523	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL437132	175523	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL412358	219765	0	None	-10	2	Human	8.0	pEC50	=	8	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)N=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44441684	100906	0	None	28	3	Human	8.0	pEC50	=	8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL249321	100906	0	None	28	3	Human	8.0	pEC50	=	8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.0	pEC50	=	8.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44448631	101845	0	None	1	4	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL255286	101845	0	None	1	4	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL5081077	221496	0	None	-89	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168295726	199184	0	None	-117	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5207936	199184	0	None	-117	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL589308	222578	0	None	-1	3	Mouse	8.0	pEC50	=	8.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N(CC(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	44394659	73728	0	None	53	3	Human	8.0	pEC50	=	8.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	754	19	9	7	1.5	N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL186687	73728	0	None	53	3	Human	8.0	pEC50	=	8.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	754	19	9	7	1.5	N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11239907	139905	0	None	-18	4	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	854	30	9	7	4.1	CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL370261	139905	0	None	-18	4	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	854	30	9	7	4.1	CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	46228690	208271	0	None	-63	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL605115	208271	0	None	-63	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	137638218	163607	0	None	-2	4	Mouse	7.0	pEC50	=	7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	988	11	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4071283	163607	0	None	-2	4	Mouse	7.0	pEC50	=	7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	988	11	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	44373317	126436	0	None	2	2	Human	7.0	pEC50	=	7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL346930	126436	0	None	2	2	Human	7.0	pEC50	=	7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	16157270	219332	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	CHEMBL405282	219332	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	16157270	219332	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	CHEMBL405282	219332	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	71459896	85314	0	None	6	2	Human	6.0	pEC50	=	6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2112064	85314	0	None	6	2	Human	6.0	pEC50	=	6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	44442998	100381	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL246631	100381	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	44443016	100863	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
	CHEMBL249064	100863	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
	CHEMBL3600921	218603	0	None	-7	4	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	11706338	208486	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237150	208486	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237166	208486	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL606399	208486	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	145966364	170899	0	None	-131	3	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4209913	170899	0	None	-131	3	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL320157	218005	0	None	-1	4	Mouse	6.0	pEC50	=	6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	11851038	147113	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44349170	123601	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	650	9	4	5	4.8	O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL337941	123601	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	650	9	4	5	4.8	O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44348844	124981	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	4.0	CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL340908	124981	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	4.0	CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL381739	219071	0	None	-8	3	Human	5.0	pEC50	=	5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0510326
	44305763	209865	0	None	-5	4	Mouse	4.0	pEC50	=	4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	3.1	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	CHEMBL63850	209865	0	None	-5	4	Mouse	4.0	pEC50	=	4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	3.1	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	164612768	191498	0	None	-165	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	591	10	3	3	6.3	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4850501	191498	0	None	-165	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	591	10	3	3	6.3	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	164613353	191554	0	None	-	1	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	539	13	4	4	4.0	CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O	10.1021/acs.jmedchem.0c02041
	CHEMBL4851292	191554	0	None	-	1	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	539	13	4	4	4.0	CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O	10.1021/acs.jmedchem.0c02041
	164613550	191908	0	None	-177	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	606	11	3	3	6.7	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4856539	191908	0	None	-177	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	606	11	3	3	6.7	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	45487298	204121	0	None	-12	4	Mouse	5.0	pEC50	=	5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	657	17	8	8	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568965	204121	0	None	-12	4	Mouse	5.0	pEC50	=	5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	657	17	8	8	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	49862663	21894	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209705	21894	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44413576	84931	0	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	725	10	10	7	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL210399	84931	0	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	725	10	10	7	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL5091245	222079	0	None	-5	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	46228814	206155	0	None	-2	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	617	10	2	6	4.9	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590955	206155	0	None	-2	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	617	10	2	6	4.9	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	137646617	164323	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4080223	164323	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44433423	95499	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL236110	95499	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	44433423	95499	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL236110	95499	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	46885368	14728	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1090484	14728	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	44275312	148185	0	None	70	2	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL384036	148185	0	None	70	2	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44394627	130859	0	None	7	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	20	8	6	2.1	CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363272	130859	0	None	7	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	20	8	6	2.1	CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	46228726	207270	0	None	-3	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598643	207270	0	None	-3	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	137646617	164323	0	None	-2	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4080223	164323	0	None	-2	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	46202892	14528	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL1089107	14528	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL1204062	14528	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL438596	220560	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44413969	87005	0	None	-24	3	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL213752	87005	0	None	-24	3	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	44310258	166197	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932908	166197	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL410091	166197	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44413968	87004	0	None	-57	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL213751	87004	0	None	-57	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL444493	220712	0	None	37	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL438596	220560	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44405911	147285	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	994	20	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL381007	147285	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	994	20	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	1337	10197	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	9808720	70996	0	None	3	2	Human	8.0	pEC50	=	8.0	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180892	70996	0	None	3	2	Human	8.0	pEC50	=	8.0	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	6918813	138149	3	None	77	4	Human	8.0	pEC50	=	8.0	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	138149	3	None	77	4	Human	8.0	pEC50	=	8.0	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL91957	222684	0	None	3	3	Human	8.0	pEC50	=	8.0	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	168278271	197894	0	None	-23	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5187932	197894	0	None	-23	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137656521	166523	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4104927	166523	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44322895	170149	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL419307	170149	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44442954	101074	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL250495	101074	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	24848995	124725	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL340355	124725	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	145973975	171436	0	None	-16	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4216654	171436	0	None	-16	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643846	118545	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287353	118545	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	90643850	118548	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287357	118548	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44405802	79635	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200270	79635	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44349055	23238	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	613	9	2	8	3.1	COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1	10.1016/s0960-894x(03)00796-0
	CHEMBL123426	23238	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	613	9	2	8	3.1	COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1	10.1016/s0960-894x(03)00796-0
	11295737	126991	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352063	126991	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	24848995	124725	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL340355	124725	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	70695694	85189	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2111251	85189	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44397652	130412	0	None	14	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL361883	130412	0	None	14	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397461	133005	0	None	16	3	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365005	133005	0	None	16	3	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44448661	101774	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254792	101774	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44442931	157169	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL395355	157169	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443027	161799	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL401488	161799	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44433384	161489	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL399801	161489	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44433384	161489	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL399801	161489	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL3287356	218094	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	137645898	164797	0	None	-27	2	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	797	10	9	8	-1.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4085584	164797	0	None	-27	2	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	797	10	9	8	-1.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	155558348	181815	0	None	-61	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567480	181815	0	None	-61	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155566298	182572	0	None	-85	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4584189	182572	0	None	-85	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL343094	218476	0	None	-6	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	44349006	121229	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	622	8	3	6	4.1	O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1	10.1016/s0960-894x(03)00796-0
	CHEMBL333368	121229	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	622	8	3	6	4.1	O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1	10.1016/s0960-894x(03)00796-0
	44397534	74042	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188142	74042	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397698	132979	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364992	132979	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	1337	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	1337	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	1337	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	46885561	14584	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089487	14584	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44441646	160867	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL398487	160867	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	122184912	129336	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601430	129336	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	46203214	14633	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL1089831	14633	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL1204064	14633	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL430843	220400	0	None	-3	3	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	16038121	113481	0	None	-8	2	Human	6.0	pEC50	=	6.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	697	10	10	7	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL3143817	113481	0	None	-8	2	Human	6.0	pEC50	=	6.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	697	10	10	7	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46885674	14731	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	3	1	3	4.3	CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090487	14731	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	3	1	3	4.3	CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137656033	165422	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4092477	165422	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL65339	222639	0	None	-1	3	Mouse	5.0	pEC50	=	5.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	90643825	118526	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	923	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287331	118526	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	923	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44394657	134242	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	745	19	10	7	0.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL366040	134242	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	745	19	10	7	0.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	137647538	164741	0	None	-891	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084765	164741	0	None	-891	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137638725	163758	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4073016	163758	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	90643844	118544	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287351	118544	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44372942	126535	0	None	-6	2	Human	5.9	pEC50	=	5.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	786	22	11	9	-1.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL347864	126535	0	None	-6	2	Human	5.9	pEC50	=	5.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	786	22	11	9	-1.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	45487417	203823	0	None	-27	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	CHEMBL567233	203823	0	None	-27	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	46885559	14582	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089484	14582	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	73347133	96247	0	None	-7	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	96247	0	None	-7	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44416122	86903	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL213284	86903	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	56679964	70446	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801096	70446	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	25129105	183798	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
	CHEMBL463047	183798	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
	168273822	197349	0	None	-7	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5180152	197349	0	None	-7	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	11328898	14732	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1090488	14732	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1204059	14732	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	122179552	128265	0	None	-2	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12	10.1021/acsmedchemlett.5b00053
	CHEMBL3582446	128265	0	None	-2	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12	10.1021/acsmedchemlett.5b00053
	1338	10579	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL438596	220560	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL184870	215830	0	None	3	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		C=CCNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11786860	73108	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185035	73108	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	71454491	85728	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113006	85728	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	44441642	161184	0	None	75	3	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL398816	161184	0	None	75	3	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	162670951	189617	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791306	189617	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	137644225	165215	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4090425	165215	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL501679	220922	0	None	-1	3	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44277299	176211	0	None	8	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	864	23	9	8	1.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL442537	176211	0	None	8	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	864	23	9	8	1.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1	10.1016/s0960-894x(02)00830-2
	145976863	170537	0	None	-6	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	879	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4205548	170537	0	None	-6	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	879	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643838	118537	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287345	118537	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	16154396	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	16197727	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	44285019	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	57514683	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	91898441	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	CHEMBL441738	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	DB04931	7090	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	44397655	74081	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188360	74081	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	10168556	70647	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	CHEMBL180366	70647	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	137641398	165095	0	None	-162	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4089162	165095	0	None	-162	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44448479	162150	0	None	9	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403420	162150	0	None	9	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	44442977	100589	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL247636	100589	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443020	100864	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL249065	100864	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL264190	217387	1	None	-30	8	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	71456245	85751	0	None	2	4	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113039	85751	0	None	2	4	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44394694	73086	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	819	21	9	6	3.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL184895	73086	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	819	21	9	6	3.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL50056	220898	2	None	-117	7	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	44394580	128926	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	19	8	6	2.0	CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359701	128926	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	19	8	6	2.0	CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	46944097	78693	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	441	6	1	5	5.3	COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC	nan
	CHEMBL1971975	78693	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	441	6	1	5	5.3	COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC	nan
	CHEMBL3287059	218077	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137644225	165215	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4090425	165215	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	45487296	204104	0	None	-10	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	635	18	8	7	0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568836	204104	0	None	-10	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	635	18	8	7	0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL3287061	218079	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	46228764	207003	0	None	-35	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL596804	207003	0	None	-35	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46885816	14678	0	None	28	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1090161	14678	0	None	28	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL2323800	216305	0	None	-79	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	45487411	203824	0	None	-46	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL567240	203824	0	None	-46	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44278193	175216	0	None	22	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	862	22	9	7	2.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL434966	175216	0	None	22	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	862	22	9	7	2.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1	10.1016/s0960-894x(02)00830-2
	9808801	67583	0	None	29	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761871	67583	0	None	29	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
	10077258	21803	0	None	15	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209253	21803	0	None	15	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	118735100	125578	0	None	26	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421677	125578	0	None	26	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	162670951	189617	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791306	189617	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL3287329	218090	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287329	218090	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL451423	220747	0	None	1	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44373198	58940	0	None	7	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL158808	58940	0	None	7	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	10213106	79201	0	None	199	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198772	79201	0	None	199	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	71449119	85743	0	None	117	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL2113028	85743	0	None	117	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
	44323032	213383	0	None	-6	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL89004	213383	0	None	-6	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11308957	76168	0	None	-6	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	868	31	9	7	4.5	CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL193151	76168	0	None	-6	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	868	31	9	7	4.5	CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	44448631	101845	0	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL255286	101845	0	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44400428	132455	0	None	-16	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	35	9	7	6.1	CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL364726	132455	0	None	-16	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	35	9	7	6.1	CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL264190	217387	1	None	-2	8	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	44394585	73540	0	None	61	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	20	9	6	2.1	C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL185868	73540	0	None	61	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	20	9	6	2.1	C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL5077095	221258	0	None	-25	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL204310	215943	0	None	-64	4	Human	6.9	pEC50	=	6.9	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/jm0510326
	44278223	105911	0	None	5	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	878	23	9	8	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL281060	105911	0	None	5	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	878	23	9	8	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1	10.1016/s0960-894x(02)00830-2
	44277301	107633	0	None	3	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29349	107633	0	None	3	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	145972289	171299	0	None	-45	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4214826	171299	0	None	-45	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643806	118523	0	None	-12	5	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	59149264	83577	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684624	83577	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929810	83577	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2069317	83577	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885862	15243	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	462	3	1	3	4.3	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL1093857	15243	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	462	3	1	3	4.3	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL2323793	216298	0	None	-17	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	137644449	165071	0	None	-3	3	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1016	12	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4088980	165071	0	None	-3	3	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1016	12	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	44404528	79283	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL199037	79283	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44404528	79283	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL199037	79283	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	44448436	102377	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257770	102377	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44443015	100821	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL248862	100821	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443031	161335	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL399112	161335	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL2323797	216302	0	None	-67	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm301253y
	155555217	181116	0	None	-812	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550976	181116	0	None	-812	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162667982	189194	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	776	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	CHEMBL4785727	189194	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	776	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	11364343	126702	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349427	126702	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL184968	215831	0	None	7	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCC(=O)OC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	145980198	173465	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	692	17	7	6	2.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4282109	173465	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	692	17	7	6	2.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	164622453	192869	0	None	-2	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	12	3	3	6.2	CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c02041
	CHEMBL4871577	192869	0	None	-2	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	12	3	3	6.2	CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c02041
	162669632	189344	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787753	189344	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44310243	175966	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932909	175966	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL440633	175966	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44394734	71331	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	791	19	9	6	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL181494	71331	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	791	19	9	6	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	162669632	189344	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787753	189344	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL434357	220431	0	None	5	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		COP(=O)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC	10.1016/j.bmcl.2004.07.046
	46232220	207833	0	None	-3	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602652	207833	0	None	-3	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487407	203747	0	None	-8	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566545	203747	0	None	-8	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	122184636	129213	0	None	-7	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600917	129213	0	None	-7	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44393888	133860	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL365636	133860	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44408253	147122	0	None	54	4	Human	7.9	pEC50	=	7.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
	CHEMBL380727	147122	0	None	54	4	Human	7.9	pEC50	=	7.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
	52940633	24923	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269570	24923	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
	11846669	87052	0	None	2	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL213956	87052	0	None	2	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	44413930	145426	0	None	6	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377620	145426	0	None	6	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	90643805	118522	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643802	118519	0	None	-14	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	10325955	172050	0	None	112	2	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL423101	172050	0	None	112	2	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	11157584	175023	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL433710	175023	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44394730	139265	0	None	42	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	21	10	7	0.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL369770	139265	0	None	42	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	21	10	7	0.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11181928	172936	0	None	-4	4	Mouse	7.8	pEC50	=	7.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	797	26	9	7	2.5	CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL426282	172936	0	None	-4	4	Mouse	7.8	pEC50	=	7.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	797	26	9	7	2.5	CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL3799094	219047	0	None	-12	5	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	44394660	73828	0	None	41	3	Human	7.8	pEC50	=	7.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	20	9	7	0.2	NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL187167	73828	0	None	41	3	Human	7.8	pEC50	=	7.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	20	9	7	0.2	NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322958	113789	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL315356	113789	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL3350396	218258	0	None	-60	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44415972	86658	0	None	141	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
	CHEMBL212332	86658	0	None	141	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
	155556954	181327	0	None	-467	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4556149	181327	0	None	-467	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	11262020	127045	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352457	127045	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	73351850	96294	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2373212	96294	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44433475	155668	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL394160	155668	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL502300	220931	0	None	-27	4	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	71459937	85750	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113038	85750	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44409206	146962	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL380437	146962	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL309213	217794	0	None	1	2	Human	5.9	pEC50	=	5.9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	11214733	127074	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352677	127074	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	122184914	129337	0	None	-51	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601432	129337	0	None	-51	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL359765	218586	0	None	-1	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44393822	130821	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363074	130821	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	46203216	15248	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093889	15248	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204067	15248	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137658158	166496	0	None	-10	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4104465	166496	0	None	-10	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487406	203673	0	None	-12	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.3	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566150	203673	0	None	-12	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.3	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	44408388	147101	0	None	36	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL380635	147101	0	None	36	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	49862376	21812	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209319	21812	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	44275192	175661	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL438286	175661	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	90643806	118523	0	None	-12	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	59149255	83703	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70693082	83703	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929809	83703	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070252	83703	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885480	14526	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089103	14526	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	46885621	14727	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1090473	14727	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1204057	14727	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	90643815	118496	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287066	118496	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	90643843	118543	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287350	118543	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287352	218093	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44405879	148012	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	946	20	9	7	3.8	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL382930	148012	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	946	20	9	7	3.8	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	44405794	168625	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	975	21	10	7	4.0	CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL414670	168625	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	975	21	10	7	4.0	CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	10030530	24371	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL125819	24371	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2004.06.059
	44393864	72970	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL184405	72970	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	10030530	24371	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125819	24371	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44413536	146707	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379959	146707	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	145971389	171412	0	None	-15	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4216242	171412	0	None	-15	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	44457043	104388	0	None	-1	5	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL270923	104388	0	None	-1	5	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	137654884	165376	0	None	-3	3	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	840	9	10	9	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4092082	165376	0	None	-3	3	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	840	9	10	9	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	155542040	179857	0	None	-758	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4519837	179857	0	None	-758	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	44394584	103345	0	None	5	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	6	2.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL263047	103345	0	None	5	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	6	2.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11387898	62822	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL162493	62822	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	11237928	171650	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL422027	171650	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44401313	19059	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184856	19059	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028956	19059	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44397633	133158	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365051	133158	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44442997	100697	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL248205	100697	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL320157	218005	0	None	-1	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44447818	102185	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL256956	102185	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	44441686	104019	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL268722	104019	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
	11592389	206171	0	None	-6	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	591	8	1	5	5.4	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591037	206171	0	None	-6	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	591	8	1	5	5.4	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1	10.1016/j.bmc.2010.01.049
	45487404	204215	0	None	-3019	5	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	18	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569694	204215	0	None	-3019	5	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	18	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	122184575	129205	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600836	129205	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	122184909	129332	0	None	6	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601427	129332	0	None	6	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44413879	145680	0	None	-50	3	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL378293	145680	0	None	-50	3	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	11851038	147113	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL433296	220415	0	None	-2	4	Mouse	6.8	pEC50	=	6.8	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44394582	175153	0	None	2	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	21	8	6	2.5	CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL434544	175153	0	None	2	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	21	8	6	2.5	CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44448698	101707	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254351	101707	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	90643842	118541	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287349	118541	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44441648	161470	0	None	41	3	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL399715	161470	0	None	41	3	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	122184637	129214	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600918	129214	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44413577	146304	0	None	-5	2	Human	5.8	pEC50	=	5.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379531	146304	0	None	-5	2	Human	5.8	pEC50	=	5.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46885325	15088	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	CHEMBL1092733	15088	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	44394626	72558	0	None	12	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	743	19	8	6	1.7	CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL183476	72558	0	None	12	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	743	19	8	6	1.7	CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44310259	168479	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932914	168479	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL413465	168479	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL413573	219854	0	None	-30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
	44408252	147447	0	None	30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL381503	147447	0	None	30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	44408189	175658	0	None	32	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
	CHEMBL438259	175658	0	None	32	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
	10373417	107582	0	None	301	2	Human	7.8	pEC50	=	7.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29317	107582	0	None	301	2	Human	7.8	pEC50	=	7.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	44444495	161694	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL400932	161694	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	9867330	104617	0	None	14	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
	CHEMBL272099	104617	0	None	14	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
	44444495	161694	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL400932	161694	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	44444497	161791	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
	CHEMBL401465	161791	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
	9960253	123727	0	None	25	2	Human	7.8	pEC50	=	7.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL338594	123727	0	None	25	2	Human	7.8	pEC50	=	7.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	71456236	85665	0	None	-31	2	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112918	85665	0	None	-31	2	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	6918813	138149	3	None	77	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	138149	3	None	77	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44413535	103480	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL264120	103480	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	44322977	118346	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL328117	118346	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	168271237	197267	0	None	-69	4	Human	7.8	pEC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5179081	197267	0	None	-69	4	Human	7.8	pEC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	155563222	182070	0	None	-524	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4572994	182070	0	None	-524	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155564058	182113	0	None	-794	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4574056	182113	0	None	-794	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	90643844	118544	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287351	118544	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44409140	148064	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL383256	148064	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	44405425	78635	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	CHEMBL197020	78635	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	44443033	100473	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL247010	100473	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL264190	217387	1	None	-30	8	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	155556466	181195	0	None	-2238	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4552764	181195	0	None	-2238	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	44349151	25302	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	603	7	3	7	2.5	COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127461	25302	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	603	7	3	7	2.5	COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44413842	145155	0	None	-3	3	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377210	145155	0	None	-3	3	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44394010	132203	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL364577	132203	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	10188529	133559	0	None	19	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL365401	133559	0	None	19	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	46228846	206172	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	567	9	1	6	4.3	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591041	206172	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	567	9	1	6	4.3	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	25133903	177337	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
	CHEMBL445009	177337	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
	CHEMBL420581	220030	0	None	-27	2	Human	5.8	pEC50	=	5.8	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44394093	134017	0	None	3	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	881	19	9	6	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365825	134017	0	None	3	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	881	19	9	6	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44456138	102128	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL256686	102128	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	145989222	174059	0	None	1	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	676	17	7	6	2.2	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4293365	174059	0	None	1	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	676	17	7	6	2.2	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	44413932	144324	0	None	3	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
	CHEMBL375440	144324	0	None	3	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
	CHEMBL3287329	218090	0	None	1	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287064	218082	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL264190	217387	1	None	-2	8	Mouse	7.8	pEC50	=	7.8	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	49862742	21742	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1208802	21742	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL264190	217387	1	None	-2	8	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	137662147	166158	0	None	25	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4100598	166158	0	None	25	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11555886	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL404696	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44443035	161196	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	CHEMBL398929	161196	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	44444493	161909	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL402058	161909	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL432201	220412	0	None	6	5	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	57817730	83698	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684622	83698	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929805	83698	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070247	83698	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	137648053	164318	0	None	-10	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	934	12	11	10	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4080169	164318	0	None	-10	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	934	12	11	10	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	44349093	175301	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	633	8	2	7	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL435410	175301	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	633	8	2	7	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL439128	220604	0	None	-52	3	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	10141778	123497	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL337351	123497	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	46232228	207802	0	None	-5	3	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	8	8	1.0	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602299	207802	0	None	-5	3	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	8	8	1.0	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487413	204030	0	None	-14	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	616	15	10	7	-0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568409	204030	0	None	-14	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	616	15	10	7	-0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358915	19849	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL1190181	19849	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL540320	19849	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	137653925	165386	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4092141	165386	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL263822	217369	0	None	-16	4	Human	6.8	pEC50	=	6.8	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
	44393886	73133	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185145	73133	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44275264	163160	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL406636	163160	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44441689	161197	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL398932	161197	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	15953838	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL188146	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL539306	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	11635265	207265	0	None	-12	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	7	1	4	4.8	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598617	207265	0	None	-12	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	7	1	4	4.8	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	44335147	11364	0	None	-4	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL102688	11364	0	None	-4	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL275303	217600	0	None	4	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	11555886	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
	CHEMBL404696	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
	10483153	67585	0	None	53	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761873	67585	0	None	53	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	44416014	86790	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL212855	86790	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	11555886	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL404696	162413	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
	145976444	170742	0	None	-6	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4207858	170742	0	None	-6	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	46885712	14843	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1091151	14843	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1204061	14843	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	46885417	15053	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092573	15053	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44456964	163469	0	None	1	4	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL406985	163469	0	None	1	4	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	16132144	216058	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	10145026	19041	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184727	19041	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028962	19041	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	44393885	131165	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363925	131165	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
	44390421	70680	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180544	70680	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
	44322923	213325	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL88630	213325	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	127047913	146702	0	None	-19	5	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799563	146702	0	None	-19	5	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL370254	218945	3	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm0490843
	44394735	130093	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361578	130093	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44278071	107220	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	704	20	9	7	-0.6	CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	CHEMBL29056	107220	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	704	20	9	7	-0.6	CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	49862426	21833	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209383	21833	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
	15953838	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188146	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL539306	74044	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL415200	219958	0	None	-20	5	Mouse	6.8	pEC50	=	6.8	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	1334	8283	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	16133814	8283	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	CHEMBL437050	8283	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	44442995	100427	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL246837	100427	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	11364326	73460	0	None	-4	2	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL185455	73460	0	None	-4	2	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	168285101	198423	0	None	-85	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5195937	198423	0	None	-85	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	45487415	204218	0	None	-218	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569697	204218	0	None	-218	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44413913	145451	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL377779	145451	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	137643023	165089	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4089119	165089	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44394787	172767	0	None	4	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	821	21	9	7	2.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL425348	172767	0	None	4	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	821	21	9	7	2.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	90643819	118497	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287070	118497	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44441633	101305	0	None	18	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL251735	101305	0	None	18	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	44456137	161900	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
	CHEMBL402017	161900	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
	49862377	21813	0	None	13	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209320	21813	0	None	13	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	49862425	21832	0	None	74	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209382	21832	0	None	74	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	49862478	21847	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209458	21847	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	46885366	14623	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	5	1	3	4.4	CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1089796	14623	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	5	1	3	4.4	CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	11787684	77049	0	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	811	27	9	7	2.9	CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL194217	77049	0	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	811	27	9	7	2.9	CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	16132144	216058	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	16133793	216058	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	44273719	216058	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	CHEMBL214332	216058	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	137631599	163305	0	None	-16	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4067967	163305	0	None	-16	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44443026	161581	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
	CHEMBL400263	161581	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
	90643802	118519	0	None	-14	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	102096778	65580	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	51351277	65580	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	53322400	65580	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	91932360	65580	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL1688111	65580	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL2323794	216299	0	None	-21	3	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44349173	123768	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/s0960-894x(03)00796-0
	CHEMBL338768	123768	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/s0960-894x(03)00796-0
	44393821	73486	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185583	73486	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL3349030	218184	0	None	-1	3	Human	6.7	pEC50	=	6.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	168285904	198449	0	None	-117	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5196407	198449	0	None	-117	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	44433380	95262	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL234992	95262	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	11341045	72940	0	None	-4	2	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
	CHEMBL184275	72940	0	None	-4	2	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
	44349110	25323	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	559	7	3	5	3.4	CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127574	25323	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	559	7	3	5	3.4	CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL264190	217387	1	None	-30	8	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	45487291	204152	0	None	-6	3	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569220	204152	0	None	-6	3	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44448480	102333	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257616	102333	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	44409379	83297	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL206018	83297	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	137647538	164741	0	None	-891	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084765	164741	0	None	-891	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287073	218088	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	49862662	21893	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209704	21893	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44441639	100825	0	None	11	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248893	100825	0	None	11	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	46232222	207834	0	None	-3	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	8	8	0.2	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602653	207834	0	None	-3	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	8	8	0.2	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643804	118521	0	None	-8	5	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	122184634	129211	0	None	-2	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600915	129211	0	None	-2	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44456957	104814	0	None	-8	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	432	5	1	2	5.2	O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21	10.1021/jm701303z
	CHEMBL273044	104814	0	None	-8	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	432	5	1	2	5.2	O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21	10.1021/jm701303z
	10373417	107582	0	None	301	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29317	107582	0	None	301	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	137638778	163537	0	None	11	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4070639	163537	0	None	11	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44447251	161577	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at MC4RAgonist activity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
	CHEMBL400237	161577	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at MC4RAgonist activity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
	127047913	146702	0	None	-4	5	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799563	146702	0	None	-4	5	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	44415918	148327	0	None	-1	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL384774	148327	0	None	-1	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	1323	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	92432	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	CHEMBL430239	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	44569175	195601	0	None	12	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
	CHEMBL506272	195601	0	None	12	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
	73347133	96247	0	None	-7	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	96247	0	None	-7	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44275656	166247	0	None	6	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	15	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL410148	166247	0	None	6	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	15	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2070242	215962	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	11753695	15165	7	None	3	8	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	15165	7	None	3	8	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	1324	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44405858	79636	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	4.2	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200276	79636	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	4.2	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405833	140235	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	877	23	10	7	2.6	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL370665	140235	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	877	23	10	7	2.6	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405836	141986	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	882	21	9	7	2.5	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372200	141986	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	882	21	9	7	2.5	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405860	142934	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	925	22	10	7	4.4	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL373259	142934	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	925	22	10	7	4.4	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	9919056	147847	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL382511	147847	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405793	165724	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1	10.1016/j.bmcl.2005.08.083
	CHEMBL409588	165724	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1	10.1016/j.bmcl.2005.08.083
	44405792	172889	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	940	23	10	7	4.1	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL425992	172889	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	940	23	10	7	4.1	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405910	177235	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL444880	177235	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200614	215887	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL		None	None	None		CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL434186	220430	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL		None	None	None		CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11273288	19732	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL1189370	19732	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL538567	19732	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	44404526	103267	0	None	346	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL262470	103267	0	None	346	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1	10.1016/j.bmcl.2005.08.012
	9919056	147847	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL382511	147847	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL3644320	218739	0	None	30	2	Human	8.7	pEC50	=	8.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	CHEMBL3646886	218803	0	None	39	2	Human	8.7	pEC50	=	8.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	CHEMBL5083551	221648	0	None	-10	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1338	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	9938402	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	CHEMBL339053	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	1338	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	9938402	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	CHEMBL339053	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	1323	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	92432	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	CHEMBL430239	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	44448629	174242	0	None	-3	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL429854	174242	0	None	-3	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	46911588	70442	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801092	70442	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	1323	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	92432	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	CHEMBL430239	9465	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	44358565	36799	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
	CHEMBL138901	36799	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	1338	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	1338	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	10579	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	118722929	123010	0	None	-2	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358538	123010	0	None	-2	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	10101361	162482	0	None	1	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL405174	162482	0	None	1	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL5078687	221359	0	None	-4	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168271934	196864	0	None	-26	4	Human	8.7	pEC50	=	8.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5172738	196864	0	None	-26	4	Human	8.7	pEC50	=	8.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
	52943061	24920	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269568	24920	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	44416135	86959	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL213566	86959	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44416135	86959	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
	CHEMBL213566	86959	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
	16132144	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	16133793	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	44273719	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	CHEMBL214332	216058	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	118722925	123007	0	None	-3	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358534	123007	0	None	-3	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	1323	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	92432	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	CHEMBL430239	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	137662147	166158	0	None	25	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4100598	166158	0	None	25	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	52945472	24921	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269569	24921	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	56676635	70461	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801127	70461	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
	11845450	145247	0	None	-51	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377465	145247	0	None	-51	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	44408286	147446	0	None	117	4	Human	8.6	pEC50	=	8.6	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL381501	147446	0	None	117	4	Human	8.6	pEC50	=	8.6	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	52941830	24927	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269574	24927	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	90643802	118519	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2115441	216047	0	None	-8	4	Human	8.6	pEC50	=	8.6	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	10078903	74794	0	None	-7	4	Mouse	8.6	pEC50	=	8.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	769	24	9	7	1.8	CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL191303	74794	0	None	-7	4	Mouse	8.6	pEC50	=	8.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	769	24	9	7	1.8	CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	16132144	216058	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	16133793	216058	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	44273719	216058	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	CHEMBL5085972	221782	0	None	-1	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
	CHEMBL5090670	222056	0	None	3	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	49862665	21896	0	None	128	2	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209707	21896	0	None	128	2	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	90643804	118521	0	None	-8	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	90643841	118540	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287348	118540	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5087839	221899	0	None	2	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44418430	90030	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
	CHEMBL218748	90030	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
	25133209	180130	0	None	19	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
	CHEMBL452710	180130	0	None	19	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
	46919520	21910	0	None	-2	6	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	21910	0	None	-2	6	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	90643804	118521	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5094168	222258	0	None	-134	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	137637656	163017	0	None	40	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4064777	163017	0	None	40	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44448660	101748	0	None	-4	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254589	101748	0	None	-4	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	1323	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	92432	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	CHEMBL430239	9465	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	90643806	118523	0	None	-12	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL448536	220738	0	None	1	4	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	CHEMBL393075	219241	0	None	-7	4	Human	8.5	pEC50	=	8.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2007.02.020
	168270124	196734	0	None	-20	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5170533	196734	0	None	-20	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	56683296	70453	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801119	70453	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	49862751	21925	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209802	21925	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	90643804	118521	0	None	-8	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	218089	0	None	-5	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643803	118520	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	16133793	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	44273719	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	16132144	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44393824	129130	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	659	13	3	5	5.7	CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL359976	129130	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	659	13	3	5	5.7	CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2004.06.059
	1338	10579	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	10579	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	10579	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL410217	219587	0	None	2	3	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44277696	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	CHEMBL29582	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	44456027	162249	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL403967	162249	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
	44413938	145717	0	None	10	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL378446	145717	0	None	10	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL3287327	218089	0	None	-5	5	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2323795	216300	0	None	-39	4	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	90643826	118527	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287333	118527	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44277696	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL29582	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	44409339	81771	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL203252	81771	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL78565	222659	0	None	-1	2	Human	7.7	pEC50	=	7.7	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44394693	103373	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	805	20	9	6	2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL263234	103373	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	805	20	9	6	2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44373177	126609	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL348511	126609	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44372933	126691	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL349298	126691	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44277696	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
	CHEMBL29582	107982	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
	CHEMBL411400	219662	0	None	-141	5	Mouse	7.7	pEC50	=	7.7	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O	10.1021/jm030452x
	44323031	174857	0	None	-39	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL432565	174857	0	None	-39	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	71452720	85746	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL2113031	85746	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	44322812	119159	0	None	-5	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL329586	119159	0	None	-5	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11491374	74394	0	None	-21	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	840	29	9	7	3.7	CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL190366	74394	0	None	-21	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	840	29	9	7	3.7	CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL501592	220920	0	None	-38	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	CHEMBL501642	220921	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL509582	222325	0	None	6	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	44405832	140362	0	None	14	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	909	21	8	7	2.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL371215	140362	0	None	14	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	909	21	8	7	2.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	11272336	63968	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164969	63968	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44397657	130901	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363384	130901	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL438235	220538	0	None	-10	3	Human	6.7	pEC50	=	6.7	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C	10.1021/jm030119t
	CHEMBL446185	220723	0	None	-5	3	Human	5.7	pEC50	=	5.7	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
	71459937	85750	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113038	85750	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44349226	123761	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL338747	123761	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	11845444	86842	0	None	-11	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL213026	86842	0	None	-11	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44413970	145793	0	None	-50	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL378571	145793	0	None	-50	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL2323792	216297	0	None	-2	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL438596	220560	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	118735103	125581	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421680	125581	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	90643833	118533	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287340	118533	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL566764	222532	0	None	-2	2	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CC(=O)N/C(=C\c1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	90643819	118497	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287070	118497	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44393889	73121	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185094	73121	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44393877	129031	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL359777	129031	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL3287064	218082	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	46885524	14576	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1089462	14576	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1204054	14576	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL264190	217387	1	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	16132144	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16132144	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL3287356	218094	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44394691	129681	0	None	15	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL360598	129681	0	None	15	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11753667	63952	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164857	63952	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44441643	161579	0	None	43	2	Human	7.7	pEC50	=	7.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL400252	161579	0	None	43	2	Human	7.7	pEC50	=	7.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	44323034	213309	0	None	-1	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL88537	213309	0	None	-1	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11263053	74795	0	None	-29	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	33	9	7	5.3	CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL191304	74795	0	None	-29	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	33	9	7	5.3	CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL88185	222675	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44444508	161861	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL401853	161861	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL526334	222460	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
	CHEMBL3287327	218089	0	None	-5	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2323529	216289	0	None	-2	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11261324	64908	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL167780	64908	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44397569	129684	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL360602	129684	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3600842	218598	0	None	-7	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL50056	220898	2	None	-117	7	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44349008	121106	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	646	10	4	7	3.1	CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL333071	121106	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	646	10	4	7	3.1	CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	137659949	165911	0	None	-1	2	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3926	63	56	62	-18.1	CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O	10.1021/acs.jmedchem.8b00251
	CHEMBL4097903	165911	0	None	-1	2	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3926	63	56	62	-18.1	CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O	10.1021/acs.jmedchem.8b00251
	52943061	24920	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269568	24920	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL50056	220898	2	None	-117	7	Mouse	5.7	pEC50	=	5.7	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	16725558	162448	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL404905	162448	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	90643847	118546	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287354	118546	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2369131	216372	0	None	-5	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44441682	161427	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL399474	161427	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	168295131	199021	0	None	-14	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5205283	199021	0	None	-14	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL3600920	218602	0	None	-8	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	52918026	67582	0	None	63	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761870	67582	0	None	63	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	11753695	15165	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093304	15165	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	11753695	15165	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	15165	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	90643847	118546	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287354	118546	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44409104	83300	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	CHEMBL206033	83300	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	44322957	212990	0	None	-3	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL86573	212990	0	None	-3	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL5075506	221158	0	None	-676	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5091236	222078	0	None	-48	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44442972	159797	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397562	159797	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	145948912	174264	0	None	-8	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL	1170	17	14	11	0.7	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
	CHEMBL4299454	174264	0	None	-8	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL	1170	17	14	11	0.7	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
	46885622	15231	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093801	15231	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL2323785	216290	0	None	-35	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL500516	220896	0	None	1	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44405913	139514	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	21	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL369915	139514	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	21	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44349134	124101	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	12	2	6	4.4	CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339708	124101	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	12	2	6	4.4	CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	90643833	118533	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287340	118533	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	46232225	207861	0	None	-6	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	8	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602852	207861	0	None	-6	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	8	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643828	118529	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287335	118529	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	90643834	118534	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287341	118534	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	118735102	125580	0	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421679	125580	0	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	10348630	36969	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL139042	36969	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	45487295	204153	0	None	-13	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	18	8	7	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569221	204153	0	None	-13	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	18	8	7	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137660671	165997	0	None	-812	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4098785	165997	0	None	-812	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137656489	166489	0	None	-1	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1125	13	13	12	-1.2	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4104402	166489	0	None	-1	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1125	13	13	12	-1.2	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL195468	215881	0	None	-7	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	44394583	129123	0	None	6	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	18	8	6	2.4	CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359927	129123	0	None	6	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	18	8	6	2.4	CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44442956	101123	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL250701	101123	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44397658	132204	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364582	132204	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	155567399	182745	0	None	-501	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4588429	182745	0	None	-501	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL3287073	218088	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL432895	220414	4	None	-1	4	Mouse	5.6	pEC50	=	5.6	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	45487288	204135	0	None	-18	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	623	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569076	204135	0	None	-18	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	623	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	45487286	204120	0	None	-41	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	631	16	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568940	204120	0	None	-41	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	631	16	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358660	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL435697	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL544851	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	44305790	109617	0	None	1	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	CHEMBL305559	109617	0	None	1	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	44305704	210116	0	None	1	4	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	CHEMBL64954	210116	0	None	1	4	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	44396986	74206	0	None	20	3	Human	6.6	pEC50	=	6.6	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL188966	74206	0	None	20	3	Human	6.6	pEC50	=	6.6	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	44278194	106146	0	None	8	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	848	22	9	7	1.9	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL282533	106146	0	None	8	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	848	22	9	7	1.9	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1	10.1016/s0960-894x(02)00830-2
	24873537	152839	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL391902	152839	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL2370964	216746	0	None	-74	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	90643830	118531	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287337	118531	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44349019	121214	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL333283	121214	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44322986	112874	0	None	-3	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL313377	112874	0	None	-3	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2370964	216746	0	None	-74	4	Human	7.6	pEC50	=	7.6	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	16132144	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	16133793	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	44273719	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL214332	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL5087814	221898	0	None	-4	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	10098133	21787	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209191	21787	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL2323790	216295	0	None	-7	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	24882615	104268	0	None	-5	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	371	6	2	3	3.1	NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O	10.1021/jm701303z
	CHEMBL270270	104268	0	None	-5	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	371	6	2	3	3.1	NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O	10.1021/jm701303z
	11157584	175023	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL433710	175023	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44358660	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL435697	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL544851	175338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	122184577	129207	0	None	-19	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600838	129207	0	None	-19	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL105113	215245	0	None	-1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	44349111	124264	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	10	2	6	4.2	CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339979	124264	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	10	2	6	4.2	CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	44397651	73725	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186675	73725	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	46885560	14583	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089485	14583	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44448628	161896	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL402009	161896	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL430489	220399	0	None	-2	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	137631599	163305	0	None	-16	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4067967	163305	0	None	-16	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	90643848	118547	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287355	118547	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	137660671	165997	0	None	-812	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4098785	165997	0	None	-812	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137658158	166496	0	None	-10	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4104465	166496	0	None	-10	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	16132144	216058	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	16133793	216058	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	44273719	216058	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	CHEMBL214332	216058	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	44413880	84721	0	None	-10	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
	CHEMBL209587	84721	0	None	-10	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
	16132144	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	16133793	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	44273719	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	CHEMBL214332	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	10257242	21802	0	None	39	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209252	21802	0	None	39	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	10077258	21803	0	None	15	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209253	21803	0	None	15	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	25132867	179277	0	None	15	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
	CHEMBL448337	179277	0	None	15	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
	CHEMBL2371888	216925	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(C)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	71452716	85668	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL2112920	85668	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL322610	218013	0	None	-2	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	16132144	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	16133793	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	44273719	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	CHEMBL214332	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	71452716	85668	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112920	85668	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL508501	221721	0	None	36	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL438596	220560	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL438596	220560	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	90643848	118547	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287355	118547	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44358630	35087	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137452	35087	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL541866	35087	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL443590	220704	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	CHEMBL311175	217877	0	None	-2	2	Human	5.6	pEC50	=	5.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	11845630	146292	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL379490	146292	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44394009	131128	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363684	131128	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	44413881	144371	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL375559	144371	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	46885324	14982	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1092210	14982	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	45487287	204428	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	633	17	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL570903	204428	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	633	17	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	46886010	14646	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1089892	14646	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137649543	164099	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4077331	164099	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	155549760	180656	0	None	-66	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4539621	180656	0	None	-66	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	1338	10579	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL2310901	216277	0	None	-4	4	Human	7.6	pEC50	=	7.6	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	CHEMBL5087859	221902	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44322959	162854	0	None	-13	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL406276	162854	0	None	-13	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11423083	103614	0	None	-26	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	882	32	9	7	4.9	CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL265236	103614	0	None	-26	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	882	32	9	7	4.9	CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL3287327	218089	0	None	-5	5	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	155539948	179665	0	None	-131	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4515666	179665	0	None	-131	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL138771	215533	0	None	1	3	Mouse	6.6	pEC50	=	6.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N(CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	44358705	103400	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL263461	103400	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	1334	8283	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16133814	8283	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL437050	8283	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	49789765	74006	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	363	4	1	5	4.7	COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1	nan
	CHEMBL1879413	74006	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	363	4	1	5	4.7	COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1	nan
	CHEMBL3600841	218597	0	None	-1	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	11845276	86828	0	None	2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
	CHEMBL212976	86828	0	None	2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
	1334	8283	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133814	8283	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL437050	8283	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	90643838	118537	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287345	118537	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44456304	162033	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	CHEMBL402787	162033	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	56676633	70455	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801121	70455	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
	16132144	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44394736	130094	0	None	25	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361579	130094	0	None	25	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44390424	70701	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180635	70701	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	137660993	166226	0	None	-63	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4101216	166226	0	None	-63	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44433448	95259	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL234983	95259	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44433448	95259	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL234983	95259	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	145966716	171084	0	None	-70	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212209	171084	0	None	-70	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL2070254	215964	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	155567887	182827	0	None	1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	676	19	10	7	-1.1	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4590532	182827	0	None	1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	676	19	10	7	-1.1	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	164623811	192679	0	None	-1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	614	11	4	4	6.2	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868636	192679	0	None	-1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	614	11	4	4	6.2	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL438596	220560	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44391940	19022	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1184624	19022	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145456	19022	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44405366	78736	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	CHEMBL197327	78736	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	11375764	73463	0	None	-38	2	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL185469	73463	0	None	-38	2	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL414778	219935	0	None	-478	4	Human	5.6	pEC50	=	5.6	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	90643850	118548	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287357	118548	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44359589	38253	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	685	20	4	7	1.4	CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	CHEMBL140324	38253	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	685	20	4	7	1.4	CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	51350911	65578	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53322399	65578	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932357	65578	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688109	65578	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	11156852	72459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL183434	72459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44394078	168496	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL413556	168496	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	90643834	118534	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287341	118534	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	56669816	70451	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801117	70451	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	25133907	183503	0	None	5	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	CHEMBL460138	183503	0	None	5	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	162672255	189650	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791788	189650	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	90643823	118498	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287074	118498	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	44323033	113929	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL316259	113929	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	162672255	189650	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791788	189650	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL5077144	221264	0	None	-13	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44441645	100902	0	None	63	3	Human	7.5	pEC50	=	7.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL249277	100902	0	None	63	3	Human	7.5	pEC50	=	7.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	137637656	163017	0	None	40	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4064777	163017	0	None	40	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	145988867	173882	0	None	-3	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	660	17	7	6	1.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4289983	173882	0	None	-3	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	660	17	7	6	1.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	133053557	170485	0	None	-15	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4204975	170485	0	None	-15	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643824	118525	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287330	118525	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643828	118529	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287335	118529	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44405378	147343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	CHEMBL381197	147343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	44305956	109538	0	None	1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	2.9	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	CHEMBL305132	109538	0	None	1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	2.9	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	44441636	100787	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248701	100787	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	11512024	207264	0	None	-5	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598616	207264	0	None	-5	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	46885326	14983	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	450	3	2	3	3.5	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1092211	14983	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	450	3	2	3	3.5	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	46228813	208228	0	None	-16	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	538	8	1	6	3.9	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL604911	208228	0	None	-16	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	538	8	1	6	3.9	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	49862378	21814	0	None	45	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209321	21814	0	None	45	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	11170774	165143	1	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay	ChEMBL	1180	19	13	12	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4089689	165143	1	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay	ChEMBL	1180	19	13	12	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	137656180	165807	0	None	-13	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1005	12	12	11	-2.0	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4096678	165807	0	None	-13	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1005	12	12	11	-2.0	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL2096759	215987	0	None	-7	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	44391927	20763	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL1196971	20763	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL3216393	20763	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL187125	215834	0	None	30	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)Nc1ccco1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL89270	222678	0	None	1	3	Human	7.5	pEC50	=	7.5	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1016/s0960-894x(03)00552-3
	73353216	96251	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2372046	96251	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	11181804	135285	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL366706	135285	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL2323789	216294	0	None	-147	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	73353216	96251	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL2372046	96251	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	11237444	134243	0	None	-5	2	Human	5.5	pEC50	=	5.5	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
	CHEMBL366042	134243	0	None	-5	2	Human	5.5	pEC50	=	5.5	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
	11845813	146582	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	CHEMBL379879	146582	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	11847312	86537	0	None	1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL211798	86537	0	None	1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL3287338	218091	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	73353216	96251	0	None	5	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2372046	96251	0	None	5	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	90643802	118519	0	None	-14	5	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL275303	217600	0	None	4	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	25128749	185249	0	None	37	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
	CHEMBL466380	185249	0	None	37	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
	73348634	96246	0	None	1	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	10	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371902	96246	0	None	1	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	10	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	90643806	118523	0	None	-12	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44405681	78568	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	2.9	C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL196773	78568	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	2.9	C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O	10.1016/j.bmcl.2005.08.083
	44405826	148049	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	21	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL383143	148049	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	21	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405857	165726	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	944	21	10	7	4.9	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL409589	165726	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	944	21	10	7	4.9	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	44401522	19556	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188041	19556	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL534928	19556	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44404522	79066	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	862	22	9	7	2.8	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198309	79066	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	862	22	9	7	2.8	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	168284256	197725	0	None	-64	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5185775	197725	0	None	-64	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	16132144	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	16133793	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	44273719	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	137659790	166101	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL4099889	166101	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1323	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	92432	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL430239	9465	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	49862749	21923	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209800	21923	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL3287327	218089	0	None	-1	5	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5094215	222260	0	None	-15	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	137637026	162704	0	None	28	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060937	162704	0	None	28	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11215553	15166	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093305	15166	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	145964017	170820	0	None	1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4208874	170820	0	None	1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643803	118520	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL438596	220560	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44441641	101076	0	None	69	3	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL250508	101076	0	None	69	3	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	16172929	219780	15	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	CHEMBL412536	219780	15	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	11215553	15166	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093305	15166	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	49862747	21920	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209798	21920	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL2371712	216888	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	CHEMBL413260	219838	0	None	5	2	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	CHEMBL5075712	221173	0	None	-102	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643805	118522	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643808	118524	0	None	-14	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	16133793	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	44273719	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	CHEMBL214332	216058	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	CHEMBL501394	220916	0	None	2	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	46919520	21910	0	None	-3	6	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	21910	0	None	-3	6	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL5090285	222032	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643805	118522	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	168272660	197212	0	None	-28	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5178164	197212	0	None	-28	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	127047475	146527	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	132991507	146527	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798421	146527	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3287338	218091	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3349030	218184	0	None	-1	3	Human	8.4	pEC50	=	8.4	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	1338	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	9938402	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	CHEMBL339053	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	44413914	146296	0	None	-12	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL379508	146296	0	None	-12	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	16132144	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	16133793	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	44273719	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	44456222	104701	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272538	104701	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	11296600	129721	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	CHEMBL360716	129721	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	56679956	70474	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801214	70474	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	49862746	21919	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209797	21919	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	90643802	118519	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11296600	129721	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360716	129721	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL5091245	222079	0	None	-5	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44441644	161617	0	None	66	3	Human	8.4	pEC50	=	8.4	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL400456	161617	0	None	66	3	Human	8.4	pEC50	=	8.4	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL322610	218013	0	None	-2	4	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	46885711	14842	0	None	123	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL1091150	14842	0	None	123	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	155543031	179960	0	None	-50	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4522298	179960	0	None	-50	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44394692	72988	0	None	17	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL184466	72988	0	None	17	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	71459938	85756	0	None	4	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113043	85756	0	None	4	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44393823	130752	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL362880	130752	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	44405450	79293	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL199061	79293	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL427205	220131	0	None	-21	3	Human	5.5	pEC50	=	5.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
	155565321	182355	0	None	-100	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4579448	182355	0	None	-100	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	168274920	197042	0	None	-102	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5175444	197042	0	None	-102	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL321870	218011	0	None	-5	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	51350799	65575	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53323763	65575	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932356	65575	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688105	65575	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44358698	37697	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL139803	37697	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	56676634	70458	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	CHEMBL1801124	70458	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	168272615	197166	0	None	-60	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5177494	197166	0	None	-60	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	137655905	165607	0	None	-74	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4094606	165607	0	None	-74	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44444507	100948	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL249571	100948	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	25132524	183537	0	None	7	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	CHEMBL460349	183537	0	None	7	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	44394690	131426	0	None	14	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL364119	131426	0	None	14	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44394658	175116	0	None	5	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	758	18	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL434329	175116	0	None	5	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	758	18	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	162672691	189980	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4795842	189980	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL5076315	221207	0	None	-3	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643837	118536	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287344	118536	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	155562237	182488	0	None	-1548	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4582276	182488	0	None	-1548	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	9852256	182146	0	None	-7	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	632	15	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4574756	182146	0	None	-7	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	632	15	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	45487300	204138	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	15	8	8	-0.6	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569086	204138	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	15	8	8	-0.6	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	44413537	146325	0	None	-2	2	Human	5.5	pEC50	=	5.5	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379627	146325	0	None	-2	2	Human	5.5	pEC50	=	5.5	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46228845	206167	0	None	-39	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	9	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591026	206167	0	None	-39	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	9	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228848	206178	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	8	0	6	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591061	206178	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	8	0	6	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228849	206190	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	595	10	0	7	4.8	CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL591123	206190	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	595	10	0	7	4.8	CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21	10.1016/j.bmc.2010.01.049
	46228847	206192	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	620	11	1	7	6.0	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL591132	206192	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	620	11	1	7	6.0	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	46228842	206195	0	None	-38	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	592	8	1	6	4.3	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591194	206195	0	None	-38	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	592	8	1	6	4.3	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1	10.1016/j.bmc.2010.01.049
	46228844	206196	0	None	-26	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	587	10	1	7	4.3	COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591195	206196	0	None	-26	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	587	10	1	7	4.3	COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228888	206266	0	None	-8	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	481	6	1	4	3.2	CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591717	206266	0	None	-8	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	481	6	1	4	3.2	CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	46228763	206965	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL596602	206965	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46228659	207172	0	None	-20	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598010	207172	0	None	-20	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228850	207206	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	544	9	2	6	3.9	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598208	207206	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	544	9	2	6	3.9	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	46228725	207236	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598442	207236	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46228841	207304	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	503	8	0	4	4.8	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598831	207304	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	503	8	0	4	4.8	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228843	208424	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	8	1	5	4.6	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL605970	208424	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	8	1	5	4.6	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	11706338	208486	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237150	208486	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237166	208486	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL606399	208486	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	11846673	86769	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL212766	86769	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	137643385	164910	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4087072	164910	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643836	118535	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287343	118535	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	56666397	70448	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801098	70448	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	162672691	189980	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4795842	189980	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	46885415	15051	0	None	10	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092571	15051	0	None	10	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL432201	220412	0	None	6	5	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44444432	101179	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL250976	101179	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	44397356	73691	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186557	73691	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44431512	152702	0	None	-87	4	Human	5.5	pEC50	=	5.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
	CHEMBL391796	152702	0	None	-87	4	Human	5.5	pEC50	=	5.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
	CHEMBL3287352	218093	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	51351024	65576	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53318435	65576	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932358	65576	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688106	65576	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	11685018	207472	0	None	-204	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL599867	207472	0	None	-204	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	11627577	207970	0	None	-4	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL603468	207970	0	None	-4	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL438596	220560	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL80803	222664	0	None	-9	2	Human	5.5	pEC50	=	5.5	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	10123761	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL283214	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	44275121	103261	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL262437	103261	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11851038	147113	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	11636019	79135	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL198535	79135	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	49862739	21913	0	None	23	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209791	21913	0	None	23	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	44401585	20535	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL1195347	20535	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL554368	20535	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	46232227	205949	0	None	-6	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589517	205949	0	None	-6	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	137660993	166226	0	None	-63	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4101216	166226	0	None	-63	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	46228660	207173	0	None	-21	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598011	207173	0	None	-21	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	90643808	118524	0	None	-14	5	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11341811	126902	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL351161	126902	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44393863	134331	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL366321	134331	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL439691	220627	0	None	-5	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	44391938	18518	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1181567	18518	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145455	18518	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44397220	174083	0	None	28	3	Human	7.5	pEC50	=	7.5	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL429387	174083	0	None	28	3	Human	7.5	pEC50	=	7.5	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL438030	220523	0	None	-21	3	Human	7.5	pEC50	=	7.5	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	CHEMBL204864	215945	0	None	-12	4	Human	6.5	pEC50	=	6.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
	44455893	162417	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL404706	162417	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL409636	219552	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm030119t
	44349228	25587	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL127861	25587	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44305770	209573	0	None	-1	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	448	9	5	4	2.2	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1	10.1016/s0960-894x(03)00318-4
	CHEMBL62228	209573	0	None	-1	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	448	9	5	4	2.2	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1	10.1016/s0960-894x(03)00318-4
	CHEMBL431242	220403	0	None	-1	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	46885713	14571	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1	10.1021/jm9017866
	CHEMBL1089442	14571	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1	10.1021/jm9017866
	44278195	105582	0	None	35	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	834	21	9	7	1.6	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL27848	105582	0	None	35	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	834	21	9	7	1.6	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1	10.1016/s0960-894x(02)00830-2
	10123761	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL283214	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	44275119	175799	0	None	37	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1033	15	11	10	1.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL439361	175799	0	None	37	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1033	15	11	10	1.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	10123761	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL283214	106269	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL185869	215832	0	None	6	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCOC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL3600843	218599	0	None	-4	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	51350673	65574	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53317148	65574	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932362	65574	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688104	65574	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	25022598	101805	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL255007	101805	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL500743	220903	0	None	-22	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	44456958	104179	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	308	4	1	2	2.8	CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21	10.1021/jm701303z
	CHEMBL269837	104179	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	308	4	1	2	2.8	CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21	10.1021/jm701303z
	49862744	21917	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209795	21917	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	11613741	206061	0	None	-223	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.7	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590281	206061	0	None	-223	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.7	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	16172929	219780	15	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL412536	219780	15	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	11181804	135285	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL366706	135285	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	145988152	173823	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4288909	173823	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	44413828	146071	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL379168	146071	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	90661465	83937	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	CHEMBL2028958	83937	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	CHEMBL2078649	83937	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	44393809	72952	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL184325	72952	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL438920	220588	0	None	-12	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	168295644	199091	0	None	1	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5206336	199091	0	None	1	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	11375529	126929	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL351400	126929	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL427629	220136	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44405365	78721	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197278	78721	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	46203213	14730	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	CHEMBL1090486	14730	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	CHEMBL1204058	14730	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	137659790	166101	0	None	-1	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4099889	166101	0	None	-1	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL5077811	221295	0	None	-87	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
	46885863	15244	0	None	41	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1093858	15244	0	None	41	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	25128751	180363	0	None	23	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
	CHEMBL453300	180363	0	None	23	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
	25128748	196770	0	None	8	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
	CHEMBL517108	196770	0	None	8	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
	44577510	195514	0	None	-15	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
	CHEMBL504986	195514	0	None	-15	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
	44275191	88664	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL216474	88664	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11330869	126758	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL349886	126758	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44349470	23705	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125308	23705	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44405426	142564	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL373037	142564	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	46884748	15168	0	None	16	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093307	15168	0	None	16	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL3350327	218249	0	None	1	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	45487410	204217	0	None	-12	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	655	16	8	6	1.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569696	204217	0	None	-12	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	655	16	8	6	1.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44448477	102332	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257615	102332	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	162643435	188446	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776340	188446	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162643435	188446	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776340	188446	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	46885416	15052	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	6	1	4	3.6	COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1092572	15052	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	6	1	4	3.6	COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	90643830	118531	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287337	118531	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL2304250	216265	0	None	-6	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44409337	177240	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL444883	177240	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	44349019	121214	0	None	-1	2	Mouse	7.4	pEC50	=	7.4	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL333283	121214	0	None	-1	2	Mouse	7.4	pEC50	=	7.4	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44394581	128927	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	19	9	6	1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359702	128927	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	19	9	6	1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322987	103507	0	None	-8	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL264306	103507	0	None	-8	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44322788	164162	0	None	-5	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL407825	164162	0	None	-5	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	90643841	118540	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287348	118540	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	155563055	182074	0	None	-75	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4573041	182074	0	None	-75	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	9960253	123727	0	None	25	2	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL338594	123727	0	None	25	2	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44349133	124062	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	3.8	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339545	124062	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	3.8	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	137634090	163078	0	None	-2	6	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3980	69	56	64	-22.2	CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2	10.1021/acs.jmedchem.8b00251
	CHEMBL4065418	163078	0	None	-2	6	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3980	69	56	64	-22.2	CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2	10.1021/acs.jmedchem.8b00251
	155512534	176471	0	None	-42	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	642	16	7	6	1.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4437801	176471	0	None	-42	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	642	16	7	6	1.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	46232221	205948	0	None	-1	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589516	205948	0	None	-1	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487290	203559	0	None	-12	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	579	17	9	7	-1.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565474	203559	0	None	-12	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	579	17	9	7	-1.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O	10.1016/j.bmcl.2009.07.025
	11846844	146857	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL380051	146857	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	44405823	79742	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	907	21	8	7	4.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200668	79742	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	907	21	8	7	4.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11421919	126759	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL349887	126759	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44394654	130751	0	None	9	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	775	20	8	7	1.7	CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL362879	130751	0	None	9	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	775	20	8	7	1.7	CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44442978	159855	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397607	159855	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44444448	100838	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL248964	100838	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL105113	215245	0	None	-1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	15953833	85749	0	None	8	4	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113037	85749	0	None	8	4	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	46865980	15240	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1093846	15240	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	25131477	185480	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
	CHEMBL468252	185480	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
	CHEMBL5075506	221158	0	None	-676	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168296647	199254	0	None	-213	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5208830	199254	0	None	-213	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	49792705	74277	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	4	1	4	5.5	CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12	nan
	CHEMBL1894685	74277	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	4	1	4	5.5	CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12	nan
	90643803	118520	0	None	-3	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	118520	0	None	-3	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	46885558	14581	0	None	151	2	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089483	14581	0	None	151	2	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	46885483	15103	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1092861	15103	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1204053	15103	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	15603023	104740	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL272660	104740	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	15602927	164661	0	None	1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL408398	164661	0	None	1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	16132144	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	16133793	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	44273719	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	44275263	168705	0	None	478	2	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	168705	0	None	478	2	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1338	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	9938402	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL339053	10579	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	44390411	70670	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL180487	70670	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	44404523	142156	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	882	22	9	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL372785	142156	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	882	22	9	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2005.08.012
	10408	7507	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	5329	7507	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	9941379	7507	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	CHEMBL2070241	7507	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	DB11653	7507	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	90643804	118521	0	None	-8	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	52944242	24925	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269572	24925	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
	56683297	70459	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	CHEMBL1801125	70459	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	90643808	118524	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643827	118528	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287334	118528	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5092761	222167	0	None	-295	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	56676631	70443	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801093	70443	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	56659468	70466	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801145	70466	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	44413931	84790	0	None	9	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL209789	84790	0	None	9	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	90643806	118523	0	None	-12	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643805	118522	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL307457	217760	0	None	-10	4	Mouse	8.4	pEC50	=	8.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL5080489	221468	0	None	1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643808	118524	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643805	118522	0	None	1	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	118522	0	None	1	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643802	118519	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	118519	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44448590	102374	0	None	25	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257759	102374	0	None	25	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	11753695	15165	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093304	15165	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	24180493	161903	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL402043	161903	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44394623	148316	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	936	26	11	8	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL384720	148316	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	936	26	11	8	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322896	174751	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL431801	174751	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	155551699	181919	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4569886	181919	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	57817763	83702	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70690940	83702	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929808	83702	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070251	83702	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	11296600	129721	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.03.053
	CHEMBL360716	129721	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.03.053
	11296600	129721	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360716	129721	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	11753695	15165	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	15165	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	44441647	161469	0	None	18	3	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL399714	161469	0	None	18	3	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	46203517	14645	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1089891	14645	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204070	14645	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	90643840	118539	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287347	118539	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287061	218079	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287063	218081	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44275263	168705	0	None	478	2	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	168705	0	None	478	2	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11238126	172127	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL423619	172127	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44393850	72871	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL183890	72871	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	10119206	125554	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL341982	125554	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.06.059
	15953833	85749	0	None	8	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113037	85749	0	None	8	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	10119206	125554	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL341982	125554	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL264190	217387	1	None	-30	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	162665450	189075	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784053	189075	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433480	95865	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL236527	95865	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	155568641	182876	0	None	-660	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4591394	182876	0	None	-660	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	162661397	188305	0	None	-70	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4765156	188305	0	None	-70	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	71457994	85354	0	None	1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	441	8	5	3	3.7	NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1	10.1016/s0960-894x(03)00318-4
	CHEMBL2112213	85354	0	None	1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	441	8	5	3	3.7	NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1	10.1016/s0960-894x(03)00318-4
	11353851	64246	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL165746	64246	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44358630	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL137452	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL541866	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	9958649	131135	0	None	-50	2	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
	CHEMBL363730	131135	0	None	-50	2	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
	71456246	85753	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113040	85753	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	71461652	85755	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113042	85755	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	45487409	203676	0	None	-6	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566162	203676	0	None	-6	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358630	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137452	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL541866	35087	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	44358697	19734	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL1189383	19734	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL538589	19734	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL317228	217979	0	None	-10	4	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)c1ccccc1	10.1021/jm010524p
	145990599	173634	0	None	-15	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4285535	173634	0	None	-15	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	168277543	197454	0	None	-102	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5181752	197454	0	None	-102	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL524861	222402	0	None	-3	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	162665450	189075	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784053	189075	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44275192	175661	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL438286	175661	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1338	10579	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	44401323	18572	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1181891	18572	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028961	18572	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44323015	118210	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL327450	118210	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44455892	104695	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL272515	104695	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
	155550083	180693	0	None	-134	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4540411	180693	0	None	-134	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44397355	133929	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365675	133929	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	11851038	147113	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL184644	215829	0	None	1	3	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	56669817	70456	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801122	70456	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
	CHEMBL361252	218613	0	None	4	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CN(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44401315	19053	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184825	19053	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028957	19053	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44322994	113774	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL315258	113774	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2323798	216303	0	None	-13	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCN)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	137658252	166408	0	None	-6	3	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	868	10	10	9	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4103508	166408	0	None	-6	3	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	868	10	10	9	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	44405368	78737	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197328	78737	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	44443022	161578	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL400249	161578	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	90643823	118498	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287074	118498	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	45487292	203631	0	None	-20	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	628	16	9	8	-0.3	N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565900	203631	0	None	-20	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	628	16	9	8	-0.3	N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL455070	220778	0	None	25	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL3287069	218086	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)c(I)c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137656521	166523	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4104927	166523	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44397660	130209	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL361731	130209	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	11692334	207207	0	None	-275	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	5	1	4	4.6	O=C1C(Cc2n[nH]c3cc(F)ccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL598214	207207	0	None	-275	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	5	1	4	4.6	O=C1C(Cc2n[nH]c3cc(F)ccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL488355	220854	0	None	-43	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(C)(C)C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44456336	162877	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	CHEMBL406309	162877	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	49862478	21847	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209458	21847	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	44409240	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	CHEMBL202699	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	44444502	161695	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL400933	161695	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44409240	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
	CHEMBL202699	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
	59077913	96245	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	845	21	8	7	2.7	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL2371886	96245	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	845	21	8	7	2.7	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44409240	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
	CHEMBL202699	81209	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
	11249788	126892	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL351088	126892	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11753668	127147	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL353239	127147	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11364802	172068	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL423250	172068	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL2370967	216749	0	None	-3	2	Human	7.4	pEC50	=	7.4	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	11599302	206148	0	None	66	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.4	COC1(Cc2n[nH]c3ccccc23)C(=O)N(CC(=O)N(c2ccc(F)cc2)C(C)C)C=CN(c2ccccc2)C1=O	10.1016/j.bmc.2010.01.049
	CHEMBL590841	206148	0	None	66	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.4	COC1(Cc2n[nH]c3ccccc23)C(=O)N(CC(=O)N(c2ccc(F)cc2)C(C)C)C=CN(c2ccccc2)C1=O	10.1016/j.bmc.2010.01.049
	CHEMBL5078687	221359	0	None	-4	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643827	118528	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287334	118528	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44349106	123656	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	623	9	3	6	3.6	CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL338274	123656	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	623	9	3	6	3.6	CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44405362	175062	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL433991	175062	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	44349105	23899	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	649	8	3	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)C(F)(F)F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL125529	23899	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	649	8	3	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)C(F)(F)F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL3287067	218084	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL184326	215828	0	None	3	3	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		COP(=S)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC	10.1016/j.bmcl.2004.07.046
	71459896	85314	0	None	6	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2112064	85314	0	None	6	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	44415991	87285	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL214770	87285	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
	44415991	87285	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
	CHEMBL214770	87285	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
	44275371	148682	0	None	10	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1032	14	11	10	0.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3N(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL386871	148682	0	None	10	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1032	14	11	10	0.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3N(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885760	15050	0	None	102	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
	CHEMBL1092550	15050	0	None	102	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
	44394783	133151	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	847	23	9	6	4.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365044	133151	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	847	23	9	6	4.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44372964	58521	0	None	20	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL158471	58521	0	None	20	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	73354716	96250	0	None	18	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL2372039	96250	0	None	18	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL5094168	222258	0	None	-134	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44433388	95347	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
	CHEMBL235432	95347	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
	44444511	100784	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL248687	100784	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44310242	163088	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932912	163088	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL406550	163088	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL364359	218701	0	None	-2	3	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NS(=O)(=O)C(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44413831	84839	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL210008	84839	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	46885815	14632	0	None	25	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL1089830	14632	0	None	25	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL3287065	218083	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	44405360	140339	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL371063	140339	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	137659790	166101	0	None	-1	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL4099889	166101	0	None	-1	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44394080	133544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL365279	133544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL3349030	218184	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	11477853	73668	0	None	-7	2	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
	CHEMBL186439	73668	0	None	-7	2	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
	46885323	14981	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092209	14981	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	51346770	65001	0	None	-29	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
	CHEMBL1682209	65001	0	None	-29	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
	137659790	166101	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4099889	166101	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137646333	164701	0	None	-13	2	Human	4.3	pEC50	=	4.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084386	164701	0	None	-13	2	Human	4.3	pEC50	=	4.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	49862425	21832	0	None	74	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209382	21832	0	None	74	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	25133207	179722	0	None	15	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
	CHEMBL451694	179722	0	None	15	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
	168277258	197489	0	None	-10	4	Human	7.3	pEC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5182345	197489	0	None	-10	4	Human	7.3	pEC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	90643808	118524	0	None	-14	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44349057	23587	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	617	8	2	7	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc(Cl)c2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL124688	23587	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	617	8	2	7	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc(Cl)c2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44397338	130455	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL362129	130455	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	45487297	203880	0	None	-9	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	613	17	8	6	0.7	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL567634	203880	0	None	-9	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	613	17	8	6	0.7	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137659394	166313	0	None	-12	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4102353	166313	0	None	-12	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	52947911	24924	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269571	24924	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL491870	220856	0	None	-9	5	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287067	218084	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44275312	148185	0	None	70	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL384036	148185	0	None	70	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11456260	163275	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL406764	163275	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44442941	159504	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397312	159504	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	71459938	85756	0	None	4	4	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113043	85756	0	None	4	4	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL311629	217879	0	None	-56	2	Human	5.3	pEC50	=	5.3	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	3794549	40889	6	None	-	1	Human	4.3	pEC50	=	4.3	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	337	3	2	5	3.7	CCc1ccc(C2CC(c3ccc(F)cc3)Nc3nc(N)nn32)cc1	nan
	CHEMBL1425554	40889	6	None	-	1	Human	4.3	pEC50	=	4.3	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	337	3	2	5	3.7	CCc1ccc(C2CC(c3ccc(F)cc3)Nc3nc(N)nn32)cc1	nan
	CHEMBL3601431	218606	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44394081	73000	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL184526	73000	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL5081077	221496	0	None	-89	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1338	10579	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	9938402	10579	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL339053	10579	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	46232226	207862	0	None	-6	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602853	207862	0	None	-6	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	71454492	85730	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113008	85730	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
	11179914	126960	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL351705	126960	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44397702	130863	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363280	130863	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3287068	218085	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	90643815	118496	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287066	118496	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287062	218080	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	122184633	129210	0	None	-4	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600914	129210	0	None	-4	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	25132864	179381	0	None	42	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
	CHEMBL449050	179381	0	None	42	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
	25132866	179390	0	None	20	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
	CHEMBL449131	179390	0	None	20	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
	CHEMBL2371880	216923	0	None	147	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(cccc3OC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885481	14527	0	None	12	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089104	14527	0	None	12	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44457067	104518	0	None	5	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL271586	104518	0	None	5	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	44405770	142226	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	22	9	7	2.9	NC(=O)CCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372829	142226	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	22	9	7	2.9	NC(=O)CCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405812	142530	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL373016	142530	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44394624	103791	0	None	-100	3	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	964	27	11	9	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL266665	103791	0	None	-100	3	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	964	27	11	9	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44401520	20702	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1196472	20702	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL557154	20702	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44401524	20778	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1197052	20778	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL559181	20778	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44404525	175435	0	None	257	2	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	864	22	10	8	2.2	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(O)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL436329	175435	0	None	257	2	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	864	22	10	8	2.2	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(O)cc2)CC1	10.1016/j.bmcl.2005.08.012
	168281389	197701	0	None	-17	4	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5185405	197701	0	None	-17	4	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
	1324	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	90643824	118525	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287330	118525	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44456102	162383	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL404549	162383	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	90643808	118524	0	None	-14	5	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-14	5	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643806	118523	0	None	-8	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-8	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44349173	123768	0	None	3	3	Human	8.3	pEC50	=	8.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
	CHEMBL338768	123768	0	None	3	3	Human	8.3	pEC50	=	8.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
	CHEMBL410672	219609	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	44408173	82176	0	None	154	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL203975	82176	0	None	154	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	145966490	171141	0	None	1	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212762	171141	0	None	1	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL3287072	218087	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	16132144	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	16133793	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	44273719	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	16132144	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	16133793	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	44273719	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	49862375	21811	0	None	16	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209318	21811	0	None	16	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	16132144	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	16133793	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	44273719	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	127047209	146590	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798845	146590	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.0c02041
	44408155	147331	0	None	114	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
	CHEMBL381125	147331	0	None	114	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
	1323	9465	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	92432	9465	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	CHEMBL430239	9465	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL503449	220945	0	None	-1	4	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137633806	163260	0	None	10	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	CHEMBL4067491	163260	0	None	10	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	44413876	86519	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	CHEMBL211699	86519	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	44413876	86519	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
	CHEMBL211699	86519	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
	127046235	146416	0	None	-10	5	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3797690	146416	0	None	-10	5	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	1338	10579	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	9938402	10579	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	CHEMBL339053	10579	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	44408190	103698	0	None	46	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL265985	103698	0	None	46	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	44408154	148140	0	None	218	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
	CHEMBL383719	148140	0	None	218	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
	155532197	178518	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1998	72	23	25	-0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4467240	178518	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1998	72	23	25	-0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	44442965	156438	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
	CHEMBL394744	156438	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
	10257242	21802	0	None	39	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209252	21802	0	None	39	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL2370968	216750	0	None	-6	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2323786	216291	0	None	-3	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44405785	79481	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL199740	79481	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44394785	130818	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	865	22	9	7	3.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363061	130818	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	865	22	9	7	3.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL2370968	216750	0	None	-6	4	Human	7.3	pEC50	=	7.3	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	168278924	197845	0	None	-33	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5187368	197845	0	None	-33	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	155531140	178397	0	None	-1	4	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	666	16	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4465466	178397	0	None	-1	4	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	666	16	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44358609	35552	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137855	35552	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	155549865	180635	0	None	-125	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	658	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4539175	180635	0	None	-125	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	658	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155561743	182551	0	None	-389	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4583714	182551	0	None	-389	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL106959	215253	0	None	-3	3	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm010524p
	1337	10197	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	11845440	145450	0	None	-4	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
	CHEMBL377778	145450	0	None	-4	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
	137640703	163876	0	None	-338	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074479	163876	0	None	-338	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487294	203592	0	None	-5	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	601	17	8	6	0.5	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565688	203592	0	None	-5	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	601	17	8	6	0.5	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	46203515	14813	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090886	14813	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204068	14813	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44393851	129867	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360989	129867	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL406891	219405	0	None	-23	5	Mouse	7.3	pEC50	=	7.3	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	44413832	84840	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL210009	84840	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	44444505	101283	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL251594	101283	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL322610	218013	0	None	-2	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	46885974	14893	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091633	14893	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	10210972	19047	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL1184771	19047	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145454	19047	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	44391929	19184	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1185810	19184	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145453	19184	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44396987	73967	0	None	22	3	Human	7.3	pEC50	=	7.3	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL187774	73967	0	None	22	3	Human	7.3	pEC50	=	7.3	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL5094215	222260	0	None	-15	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44348845	123658	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL338277	123658	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	45487414	204060	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568577	204060	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137636965	162995	0	None	-5	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4064433	162995	0	None	-5	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487405	204216	0	None	-43	3	Mouse	4.3	pEC50	=	4.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	587	16	8	6	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569695	204216	0	None	-43	3	Mouse	4.3	pEC50	=	4.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	587	16	8	6	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	56659465	70444	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801094	70444	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	46202891	14479	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	CHEMBL1088830	14479	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	CHEMBL1204060	14479	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	11851038	147113	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44275488	165906	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL409786	165906	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	44322924	113889	0	None	-7	3	Human	7.3	pEC50	=	7.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL316038	113889	0	None	-7	3	Human	7.3	pEC50	=	7.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2370965	216747	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	CHEMBL204263	215942	0	None	-87	4	Human	6.3	pEC50	=	6.3	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
	44349461	23668	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125079	23668	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44405361	141815	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	CHEMBL371945	141815	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	11635051	207175	0	None	-2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598021	207175	0	None	-2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	44413829	84841	0	None	-1	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL210011	84841	0	None	-1	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL3287060	218078	0	None	1	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2323791	216296	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44441685	100907	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249322	100907	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL264190	217387	1	None	-30	8	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	46885367	14624	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089797	14624	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44397653	73766	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186876	73766	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397412	74085	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188395	74085	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44404529	79202	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	749	18	8	6	2.0	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198776	79202	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	749	18	8	6	2.0	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	73347133	96247	0	None	-7	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	96247	0	None	-7	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44441683	100905	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249320	100905	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	44449216	102046	0	None	2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL256286	102046	0	None	2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	90643836	118535	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287343	118535	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL2369485	216407	0	None	-3	4	Mouse	7.2	pEC50	=	7.2	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44441687	100780	0	None	43	2	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL248671	100780	0	None	43	2	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44442934	100543	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL247422	100543	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	10098568	21790	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209194	21790	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	90643829	118530	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287336	118530	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2112008	216005	0	None	-1	3	Human	6.2	pEC50	=	6.2	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	44405526	79184	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL198723	79184	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL194552	215878	0	None	-1	2	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	44393862	130459	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL362147	130459	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	54584302	67586	0	None	28	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761874	67586	0	None	28	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
	44394784	133073	0	None	-2	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	861	23	9	7	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365019	133073	0	None	-2	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	861	23	9	7	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL5093939	222237	0	None	-77	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5075712	221173	0	None	-102	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44443014	160789	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL398409	160789	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	11296732	150591	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	CHEMBL390130	150591	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	164624627	192658	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868223	192658	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	44358848	125762	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL342470	125762	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL50056	220898	2	None	-4	7	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm060384p
	24848995	124725	0	None	1	2	Mouse	7.2	pEC50	=	7.2	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL340355	124725	0	None	1	2	Mouse	7.2	pEC50	=	7.2	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL183733	215826	0	None	-4	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL50056	220898	2	None	-4	7	Human	7.2	pEC50	=	7.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44442942	100374	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL246605	100374	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44405377	78799	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197541	78799	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	44456183	104798	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272956	104798	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	44275488	165906	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL409786	165906	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885759	15048	0	None	95	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	CHEMBL1092548	15048	0	None	95	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	46885482	15102	0	None	81	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092860	15102	0	None	81	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44404524	142854	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	907	24	9	8	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC(C)C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL373212	142854	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	907	24	9	8	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC(C)C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	6918813	138149	3	None	77	4	Human	8.2	pEC50	=	8.2	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	138149	3	None	77	4	Human	8.2	pEC50	=	8.2	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL217584	216156	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44408276	82282	0	None	61	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL204308	82282	0	None	61	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	90643804	118521	0	None	-8	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	118521	0	None	-8	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	218089	0	None	-5	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	71449047	85255	0	None	28	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
	CHEMBL2111807	85255	0	None	28	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
	16132144	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	16133793	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	44273719	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL214332	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	137638725	163758	0	None	3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4073016	163758	0	None	3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287060	218078	0	None	1	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44348200	166975	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
	CHEMBL410949	166975	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
	44322787	112741	0	None	1	3	Human	8.2	pEC50	=	8.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL312998	112741	0	None	1	3	Human	8.2	pEC50	=	8.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	137647009	164633	0	None	30	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4083755	164633	0	None	30	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	1324	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16154396	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16197727	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	44285019	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	57514683	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	91898441	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL441738	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	DB04931	7090	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	49862377	21813	0	None	13	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209320	21813	0	None	13	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	44441681	100904	0	None	104	2	Human	8.2	pEC50	=	8.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249319	100904	0	None	104	2	Human	8.2	pEC50	=	8.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44444510	161911	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL402060	161911	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	11851038	147113	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL3287342	218092	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	145975465	170728	0	None	6	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4207725	170728	0	None	6	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	145964837	171126	0	None	1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212629	171126	0	None	1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL5080784	221485	0	None	-2	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44444500	100919	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL249370	100919	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	54584301	67584	0	None	24	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
	CHEMBL1761872	67584	0	None	24	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
	10101361	162482	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL405174	162482	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44373197	126251	0	None	-16	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL345234	126251	0	None	-16	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44390423	70538	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180157	70538	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL5085972	221782	0	None	-1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
	168290510	198676	0	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5199932	198676	0	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	44277301	107633	0	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29349	107633	0	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	44349094	24709	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	589	9	3	6	3.0	COCC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL125935	24709	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	589	9	3	6	3.0	COCC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	155547842	180475	0	None	-251	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	741	17	10	7	-1.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4535510	180475	0	None	-251	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	741	17	10	7	-1.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155556047	181276	0	None	-199	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4554828	181276	0	None	-199	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162669064	189516	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	684	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	CHEMBL4789938	189516	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	684	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	1337	10197	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	10197	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	10197	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	137636677	162879	0	None	-75	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4063111	162879	0	None	-75	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487408	203633	0	None	-16	3	Mouse	4.2	pEC50	=	4.2	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	CHEMBL565927	203633	0	None	-16	3	Mouse	4.2	pEC50	=	4.2	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	46885907	14812	0	None	104	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090885	14812	0	None	104	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44397410	131137	0	None	31	3	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363740	131137	0	None	31	3	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	168285801	198260	0	None	-12	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
	CHEMBL5193501	198260	0	None	-12	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
	57817773	83700	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684623	83700	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929806	83700	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070249	83700	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885761	14800	0	None	56	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
	CHEMBL1090813	14800	0	None	56	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
	CHEMBL3287063	218081	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2448525	217278	0	None	-95	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	46885817	14679	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	3	1	3	4.3	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1090162	14679	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	3	1	3	4.3	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	44390422	70242	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL179837	70242	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL5077811	221295	0	None	-87	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
	137648144	164537	0	None	38	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4082585	164537	0	None	38	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL455826	220788	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44397459	132572	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364789	132572	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL413439	219849	0	None	-64	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	2891887	62148	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	CHEMBL1380969	62148	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	CHEMBL1619128	62148	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	44393820	73452	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185427	73452	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	46232223	205943	0	None	-2	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	9	8	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589468	205943	0	None	-2	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	9	8	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643839	118538	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	7	2	5	3.7	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287346	118538	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	7	2	5	3.7	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL138212	215531	0	None	-11	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O	10.1016/j.bmcl.2003.08.078
	46203212	15049	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	CHEMBL1092549	15049	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	CHEMBL1204063	15049	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	73354704	96249	0	None	13	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	989	13	11	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371913	96249	0	None	13	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	989	13	11	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44275654	164113	0	None	5	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	11	9	0.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL407754	164113	0	None	5	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	11	9	0.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	73350149	96228	0	None	2	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2371220	96228	0	None	2	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	10146483	70952	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	CHEMBL180854	70952	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	1334	8283	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16133814	8283	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL437050	8283	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	53318436	65577	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	814	17	10	9	-0.4	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O	10.1021/jm101425m
	CHEMBL1688108	65577	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	814	17	10	9	-0.4	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O	10.1021/jm101425m
	164619151	192333	0	None	-2	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	610	11	4	4	5.5	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4863206	192333	0	None	-2	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	610	11	4	4	5.5	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	44349183	25307	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	632	8	4	7	3.7	CCOC(=O)NC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127491	25307	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	632	8	4	7	3.7	CCOC(=O)NC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	155549385	180584	0	None	-117	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4538225	180584	0	None	-117	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL3287342	218092	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643826	118527	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287333	118527	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3600922	218604	0	None	-9	4	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	71456245	85751	0	None	2	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113039	85751	0	None	2	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	46228815	206141	0	None	-52	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	556	8	1	6	4.1	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590794	206141	0	None	-52	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	556	8	1	6	4.1	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	44443021	100896	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL249267	100896	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL302703	217693	0	None	-20	5	Mouse	5.2	pEC50	=	5.2	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44444504	161696	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL400934	161696	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44448515	162223	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403834	162223	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
	122184910	129333	0	None	-2	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601428	129333	0	None	-2	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	10008561	21788	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209192	21788	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	164628926	193292	0	None	-3	3	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	543	14	3	3	6.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C	10.1021/acs.jmedchem.0c02041
	CHEMBL4877537	193292	0	None	-3	3	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	543	14	3	3	6.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C	10.1021/acs.jmedchem.0c02041
	137636428	162819	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4062443	162819	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL319871	218003	0	None	-5	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	44394586	133557	0	None	7	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	759	20	8	7	1.0	COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365385	133557	0	None	7	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	759	20	8	7	1.0	COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL3287072	218087	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44349056	23578	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	651	8	2	7	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL124633	23578	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	651	8	2	7	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44397570	129687	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL360603	129687	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	137649543	164099	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4077331	164099	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	46203516	14860	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091281	14860	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204069	14860	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	46885972	14891	0	None	10	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091631	14891	0	None	10	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44349107	123657	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	637	10	2	6	3.2	CCN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL338275	123657	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	637	10	2	6	3.2	CCN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	90643832	118532	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287339	118532	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	51346771	65000	0	None	-57	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
	CHEMBL1682208	65000	0	None	-57	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
	44275372	103508	0	None	67	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	14	11	9	2.0	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3C(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL264337	103508	0	None	67	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	14	11	9	2.0	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3C(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44275175	175612	0	None	186	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1047	15	11	10	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OC(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL437822	175612	0	None	186	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1047	15	11	10	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OC(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885523	14575	0	None	263	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL1089461	14575	0	None	263	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	11226756	126752	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349850	126752	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401530	19567	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188092	19567	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL535152	19567	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44401528	20761	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1196956	20761	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL558787	20761	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	11226756	126752	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL349850	126752	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	16132144	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	168283616	198018	0	None	-13	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5190042	198018	0	None	-13	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	127047853	146771	0	None	-4	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799955	146771	0	None	-4	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	49862743	21916	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209794	21916	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL3287329	218090	0	None	-1	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643829	118530	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287336	118530	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44323029	213960	0	None	1	3	Human	8.1	pEC50	=	8.1	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL92481	213960	0	None	1	3	Human	8.1	pEC50	=	8.1	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	137648144	164537	0	None	38	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4082585	164537	0	None	38	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643808	118524	0	None	-7	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	118524	0	None	-7	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1338	10579	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	9938402	10579	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL339053	10579	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL103817	215238	0	None	2	4	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity of compound towards mouse Melanocortin-4 receptor (mMC4R); partial agonistAgonist activity of compound towards mouse Melanocortin-4 receptor (mMC4R); partial agonist	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	122179551	128264	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL3582445	128264	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL311750	217880	0	None	-4	2	Human	7.2	pEC50	=	7.2	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC/N=C(/N)NC#N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	CHEMBL411359	219658	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	44357786	123532	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL337571	123532	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL589515	222579	0	None	2	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2009.12.010
	CHEMBL2323788	216293	0	None	-13	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11613526	207267	0	None	-23	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598631	207267	0	None	-23	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	11295536	64314	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL166328	64314	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11757528	21789	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209193	21789	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	90643840	118539	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287347	118539	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44397654	73962	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL187761	73962	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397460	132997	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365004	132997	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	1334	8283	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16133814	8283	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL437050	8283	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	44335147	11364	0	None	-4	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL102688	11364	0	None	-4	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	46203215	15242	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1093856	15242	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1204065	15242	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44405769	79693	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	957	20	8	7	4.5	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL200449	79693	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	957	20	8	7	4.5	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	44393887	73448	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185417	73448	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	16132144	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	16133793	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	44273719	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	CHEMBL214332	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	145971673	171477	0	None	-12	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	837	11	12	9	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4217191	171477	0	None	-12	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	837	11	12	9	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL264190	217387	1	None	-30	8	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137643023	165089	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4089119	165089	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	46885369	14729	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	5	1	3	4.6	CC(C)CN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1090485	14729	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	5	1	3	4.6	CC(C)CN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	1334	8283	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133814	8283	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL437050	8283	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	49862740	21914	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209792	21914	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	137643385	164910	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4087072	164910	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44433385	95830	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL236489	95830	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44349594	123600	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	699	11	0	6	4.5	CC(C)(C)CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL337940	123600	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	699	11	0	6	4.5	CC(C)(C)CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL4299612	220373	0	None	-6	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.5b01894
	44442944	100375	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL246606	100375	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	71456246	85753	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113040	85753	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	137640703	163876	0	None	-338	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074479	163876	0	None	-338	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287062	218080	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44397659	73893	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL187450	73893	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3287068	218085	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2323796	216301	0	None	-691	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL312357	217888	0	None	1	2	Human	6.1	pEC50	=	6.1	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	122179549	128262	0	None	-1	2	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1021/acsmedchemlett.5b00053
	CHEMBL3582443	128262	0	None	-1	2	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1021/acsmedchemlett.5b00053
	44372908	126611	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	784	22	10	8	-0.4	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL348526	126611	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	784	22	10	8	-0.4	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	11050211	41596	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL143131	41596	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
	90643846	118545	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287353	118545	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	49862664	21895	0	None	60	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209706	21895	0	None	60	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44442981	159857	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397608	159857	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	102096778	65580	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	51351277	65580	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53322400	65580	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932360	65580	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688111	65580	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44456410	104214	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL270015	104214	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	90643843	118543	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287350	118543	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	137636428	162819	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4062443	162819	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL264190	217387	1	None	-30	8	Human	6.1	pEC50	=	6.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
	46228689	206998	0	None	-12	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL596794	206998	0	None	-12	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	25132526	195702	0	None	69	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
	CHEMBL507876	195702	0	None	69	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
	44413830	84725	0	None	-1	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL209622	84725	0	None	-1	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL2371887	216924	0	None	52	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(CC)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44409103	146901	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
	CHEMBL380120	146901	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
	11330992	126712	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349515	126712	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401310	19557	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188043	19557	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL534930	19557	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	71458041	85666	0	None	-1	2	Human	8.1	pEC50	=	8.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	776	22	10	9	-0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112919	85666	0	None	-1	2	Human	8.1	pEC50	=	8.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	776	22	10	9	-0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	168284733	198403	0	None	-35	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5195641	198403	0	None	-35	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL3287329	218090	0	None	1	5	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	49862741	21915	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209793	21915	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
	1338	10579	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	10579	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	10579	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL181161	215759	0	None	10	3	Human	8.1	pEC50	=	8.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44408275	82194	0	None	47	4	Human	8.1	pEC50	=	8.1	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL204078	82194	0	None	47	4	Human	8.1	pEC50	=	8.1	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	1323	9465	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	92432	9465	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL430239	9465	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	71461649	85729	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113007	85729	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL510687	222366	0	None	3	4	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44415919	148366	0	None	-4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL385000	148366	0	None	-4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	10864861	121978	4	None	128	2	Human	8.1	pEC50	=	8.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL334457	121978	4	None	128	2	Human	8.1	pEC50	=	8.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL602651	222597	0	None	1	3	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	16132144	216058	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	16133793	216058	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	44273719	216058	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL214332	216058	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL411378	219660	0	None	-16	5	Mouse	8.1	pEC50	=	8.1	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1	10.1021/jm030452x
	24848995	124725	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL340355	124725	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	24848995	124725	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL340355	124725	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	155548791	180509	0	None	-100	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	664	14	6	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4536340	180509	0	None	-100	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	664	14	6	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44415956	148734	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
	CHEMBL387246	148734	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
	44415956	148734	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	CHEMBL387246	148734	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	46885414	14984	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	5	1	3	4.4	C[C@H]1CN(C(=O)[C@H]2CN(CC3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092219	14984	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	5	1	3	4.4	C[C@H]1CN(C(=O)[C@H]2CN(CC3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44405375	147130	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
	CHEMBL380769	147130	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
	90643806	118523	0	None	-12	5	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	118523	0	None	-12	5	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	46885526	14536	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1089135	14536	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1204056	14536	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	44394695	129936	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	833	22	9	6	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361253	129936	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	833	22	9	6	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44392015	19550	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1187982	19550	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL3216179	19550	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44358566	171662	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL422109	171662	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	164627532	193387	0	None	-18	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	11	3	3	6.1	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4878922	193387	0	None	-18	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	11	3	3	6.1	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL3287065	218083	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	44441637	100824	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248892	100824	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	25132525	183504	0	None	3	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
	CHEMBL460142	183504	0	None	3	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
	CHEMBL263878	217377	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44349593	125167	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL341055	125167	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL2304248	216264	0	None	-4	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	137636677	162879	0	None	-75	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4063111	162879	0	None	-75	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL2304246	216262	0	None	-1	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44441688	101129	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL250719	101129	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44442943	161460	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL399667	161460	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	122184911	129334	0	None	-1	4	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601429	129334	0	None	-1	4	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	46942512	79098	0	None	-	1	Human	4.1	pEC50	=	4.1	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	1	4	5.0	CC(=O)Nc1cc(-c2cccnc2)cn2c(-c3cccc(C(F)(F)F)c3)cnc12	nan
	CHEMBL1984089	79098	0	None	-	1	Human	4.1	pEC50	=	4.1	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	1	4	5.0	CC(=O)Nc1cc(-c2cccnc2)cn2c(-c3cccc(C(F)(F)F)c3)cnc12	nan
	59149266	83701	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70693081	83701	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929807	83701	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070250	83701	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885906	15247	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093888	15247	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204066	15247	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	51351151	65579	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53318437	65579	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932359	65579	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688110	65579	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44405825	147708	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL382273	147708	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL5092761	222167	0	None	-295	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16157270	219332	14	None	-575	7	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/acs.jmedchem.5b01894
	CHEMBL405282	219332	14	None	-575	7	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/acs.jmedchem.5b01894
	137641157	163843	0	None	-24	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074074	163843	0	None	-24	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL2070374	215966	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	9919056	78848	0	None	14	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL197695	78848	0	None	14	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL183315	215822	0	None	6	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44448554	162151	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403421	162151	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44359591	38849	0	None	-1	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	699	19	8	7	-0.2	CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	CHEMBL140847	38849	0	None	-1	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	699	19	8	7	-0.2	CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	46885525	14535	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1089134	14535	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1204055	14535	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	16132144	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	216058	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	90643832	118532	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287339	118532	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44349469	23865	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125492	23865	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	137647009	164633	0	None	30	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4083755	164633	0	None	30	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11156852	72459	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	CHEMBL183434	72459	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	44416152	87873	0	None	15	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215576	87873	0	None	15	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44444499	161792	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL401466	161792	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	25129108	179475	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
	CHEMBL450236	179475	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
	11847001	87003	0	None	125	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL213747	87003	0	None	125	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44275263	168705	0	None	478	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	168705	0	None	478	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	7090	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	10169912	79200	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198771	79200	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL410168	219583	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44456184	162267	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL404069	162267	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	49862375	21811	0	None	16	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209318	21811	0	None	16	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	16132144	216058	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	16133793	216058	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	44273719	216058	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL214332	216058	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	137635422	162689	0	None	30	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060816	162689	0	None	30	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4299619	220374	0	None	-4	4	Mouse	8.0	pEC50	=	8.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL266288	103738	0	None	-	1	Mouse	8.0	pEC50	=	8.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	5507	70	67	87	-15.6	CSCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CSSSSC[C@@H]3NC(=O)[C@@H]4CCCN4C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](CSSSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(N)=O)NC1=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CSSSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N4)NC3=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSSSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCN=C(N)N)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/jm0303608
	11851038	147113	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL438596	220560	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	137637026	162704	0	None	28	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060937	162704	0	None	28	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643837	118536	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287344	118536	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11017471	38691	0	None	295	2	Human	8.0	pEC50	=	8.0	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
	CHEMBL140738	38691	0	None	295	2	Human	8.0	pEC50	=	8.0	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
	49862378	21814	0	None	45	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209321	21814	0	None	45	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL264190	217387	1	None	-30	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	49862738	21912	0	None	36	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209790	21912	0	None	36	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	56673304	70454	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801120	70454	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
	44277300	108129	0	None	16	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	850	22	9	8	1.3	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29693	108129	0	None	16	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	850	22	9	8	1.3	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC)C1	10.1016/s0960-894x(02)00830-2
	155553683	180962	0	None	-295	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4547556	180962	0	None	-295	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL3287060	218078	0	None	-1	5	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	11851038	147113	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	147113	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44405791	175430	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL436296	175430	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44393876	129345	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360169	129345	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	155551195	180721	0	None	-426	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	626	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4541098	180721	0	None	-426	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	626	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155560756	181864	0	None	-177	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4568647	181864	0	None	-177	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	122184635	129212	0	None	-56	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600916	129212	0	None	-56	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44444509	100743	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL248435	100743	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	46885973	14892	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	490	4	1	3	5.0	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(Cl)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091632	14892	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	490	4	1	3	5.0	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(Cl)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44401319	19054	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184826	19054	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028959	19054	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44393808	72905	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL184068	72905	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44394079	133543	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL365278	133543	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	137636965	162995	0	None	-5	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4064433	162995	0	None	-5	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	163196518	198908	2	None	-28	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5203580	198908	2	None	-28	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	145980719	173275	0	None	-5	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4278563	173275	0	None	-5	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	11353522	63956	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164884	63956	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401321	18568	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1181867	18568	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028960	18568	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	46884747	15167	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093306	15167	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	11308184	71673	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL182231	71673	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL410795	219621	0	None	-1	3	Human	6.0	pEC50	=	6.0	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	137656033	165422	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4092477	165422	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	122184638	129215	0	None	-18	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600919	129215	0	None	-18	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	49862737	21911	0	None	10	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209789	21911	0	None	10	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	137645483	164397	0	None	-2	3	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	906	11	11	10	-1.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4081092	164397	0	None	-2	3	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	906	11	11	10	-1.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	44413592	85192	0	None	-1	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL211131	85192	0	None	-1	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	44394786	130858	0	None	-2	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	883	22	9	7	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363271	130858	0	None	-2	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	883	22	9	7	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	90643842	118541	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287349	118541	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	46885861	15241	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	434	3	1	3	4.0	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1093855	15241	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	434	3	1	3	4.0	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	5005059	31393	4	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	514	3	3	4	6.1	O=C1C2=C(N=C(S)NC2c2ccc(Cl)cc2)NC(c2ccc(Cl)cc2)N1c1ccc(Cl)cc1	nan
	CHEMBL1343101	31393	4	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	514	3	3	4	6.1	O=C1C2=C(N=C(S)NC2c2ccc(Cl)cc2)NC(c2ccc(Cl)cc2)N1c1ccc(Cl)cc1	nan
	CHEMBL2323799	216304	0	None	-64	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11845438	144401	0	None	5	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL375775	144401	0	None	5	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	11490215	63928	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164671	63928	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL2323787	216292	0	None	-48	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL602650	222596	0	None	-2	3	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N(CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	11845804	86333	0	None	-123	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL211419	86333	0	None	-123	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	71461643	85664	0	None	-194	2	Human	6.7	pED50	=	6.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	799	22	9	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112917	85664	0	None	-194	2	Human	6.7	pED50	=	6.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	799	22	9	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	3706223	66741	10	None	-	1	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	387	8	1	4	5.6	COc1ccccc1C1(CCNC(C)c2cccs2)CCOC(C(C)C)C1	nan
	CHEMBL1733168	66741	10	None	-	1	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	387	8	1	4	5.6	COc1ccccc1C1(CCNC(C)c2cccs2)CCOC(C(C)C)C1	nan
	9842665	163585	12	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4RAntagonist activity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
	CHEMBL40711	163585	12	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4RAntagonist activity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
	9842665	163585	12	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	2948635	43491	13	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	324	4	0	5	3.5	O=C1OCCC1Sc1nc2ccccc2n1Cc1ccccc1	nan
	CHEMBL1449356	43491	13	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	324	4	0	5	3.5	O=C1OCCC1Sc1nc2ccccc2n1Cc1ccccc1	nan
	CHEMBL3752534	218995	1	None	-213	4	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL3752534	218995	1	None	-213	4	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL267492	217503	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	16007285	87897	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	CHEMBL215659	87897	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	24687534	42397	6	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	519	8	2	8	2.7	CC(C)CN(C(=O)COC(=O)c1cnc(Cl)c(Cl)c1)c1c(N)n(Cc2ccccc2)c(=O)[nH]c1=O	nan
	CHEMBL1439680	42397	6	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	519	8	2	8	2.7	CC(C)CN(C(=O)COC(=O)c1cnc(Cl)c(Cl)c1)c1c(N)n(Cc2ccccc2)c(=O)[nH]c1=O	nan
	49792747	74167	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	479	11	1	7	4.0	CCc1nc2ccc(C(=O)NCc3ccc4c(c3)OCO4)cn2c1N(CCC(C)C)CCN(C)C	nan
	CHEMBL1887976	74167	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	479	11	1	7	4.0	CCc1nc2ccc(C(=O)NCc3ccc4c(c3)OCO4)cn2c1N(CCC(C)C)CCN(C)C	nan
	44202220	66690	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	437	5	1	5	4.7	COc1ccc2sc(-c3ccc(S(C)(=O)=O)cc3)c(-c3ccc(C(N)=O)cc3)c2c1	nan
	CHEMBL1731117	66690	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	437	5	1	5	4.7	COc1ccc2sc(-c3ccc(S(C)(=O)=O)cc3)c(-c3ccc(C(N)=O)cc3)c2c1	nan
	16437205	38777	9	None	2	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	486	6	1	7	2.7	CCC1CCCCN1S(=O)(=O)c1ccc(NC(=O)c2nc(S(C)(=O)=O)ncc2Cl)cc1	nan
	CHEMBL1407961	38777	9	None	2	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	486	6	1	7	2.7	CCC1CCCCN1S(=O)(=O)c1ccc(NC(=O)c2nc(S(C)(=O)=O)ncc2Cl)cc1	nan
	2140504	59610	20	None	1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	344	4	1	6	3.4	N#Cc1cc2c(nc1SCC(=O)Nc1nccs1)CCCCC2	nan
	CHEMBL1595336	59610	20	None	1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	344	4	1	6	3.4	N#Cc1cc2c(nc1SCC(=O)Nc1nccs1)CCCCC2	nan
	1080132	37044	9	None	1	4	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	4	1	5	2.5	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1	nan
	CHEMBL1391094	37044	9	None	1	4	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	4	1	5	2.5	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1	nan
	10077594	82365	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL204670	82365	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL267492	217503	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	5662106	29286	8	None	-1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	257	4	0	4	2.8	CN(C)c1ccc(-n2cccc2/C=C/[N+](=O)[O-])cc1	nan
	CHEMBL1325640	29286	8	None	-1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	257	4	0	4	2.8	CN(C)c1ccc(-n2cccc2/C=C/[N+](=O)[O-])cc1	nan
	162674869	190093	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4797266	190093	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	1486292	41091	22	None	1	2	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	319	4	1	4	2.1	O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl	nan
	CHEMBL1427185	41091	22	None	1	2	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	319	4	1	4	2.1	O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl	nan
	162674869	190093	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4797266	190093	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	3761713	53011	6	None	-4	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	475	5	2	7	5.8	COc1ccc(OC)c(C2C3=C(O)CCCC3=NC(C)=C2C(=O)Nc2nc3ccccc3s2)c1	nan
	CHEMBL1534919	53011	6	None	-4	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	475	5	2	7	5.8	COc1ccc(OC)c(C2C3=C(O)CCCC3=NC(C)=C2C(=O)Nc2nc3ccccc3s2)c1	nan
	1316704	51713	6	None	9	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	0	3	4.8	C[S+]([O-])c1nc(-c2ccc(Br)cc2)cc(-c2ccccc2)c1C#N	nan
	CHEMBL1523206	51713	6	None	9	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	0	3	4.8	C[S+]([O-])c1nc(-c2ccc(Br)cc2)cc(-c2ccccc2)c1C#N	nan
	10324857	82767	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL205468	82767	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	44442997	100697	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL248205	100697	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	16007264	86495	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	CHEMBL211564	86495	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	16007264	86495	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
	CHEMBL211564	86495	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
	CHEMBL267492	217503	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	1189526	34739	8	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	5	0	5	3.3	O=C(C[S+]([O-])c1ccc(C(F)(F)F)cc1[N+](=O)[O-])Oc1ccccc1	nan
	CHEMBL1372179	34739	8	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	5	0	5	3.3	O=C(C[S+]([O-])c1ccc(C(F)(F)F)cc1[N+](=O)[O-])Oc1ccccc1	nan
	392617	66994	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1717770	66994	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1740201	66994	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1724806	66520	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL		None	None	None		None	nan
	2126229	41165	6	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	360	7	1	7	1.6	Cc1ccc(CNC(=O)COC(=O)Cn2nc(C)c([N+](=O)[O-])c2C)cc1	nan
	CHEMBL1427945	41165	6	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	360	7	1	7	1.6	Cc1ccc(CNC(=O)COC(=O)Cn2nc(C)c([N+](=O)[O-])c2C)cc1	nan
	44577093	185425	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL467587	185425	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	44577094	185426	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL467588	185426	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	10050686	82791	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL205553	82791	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	44447849	162245	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403938	162245	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
	21773133	79628	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	460	3	1	6	4.5	CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	CHEMBL2002430	79628	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	460	3	1	6	4.5	CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	2713	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5353524	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5360566	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	88536661	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	9552079	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL1330113	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL790	212050	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	1831123	27621	8	None	-1	3	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	489	3	1	7	5.2	Cc1nc2c(sc3nc(N4CCOCC4)c4c(c32)CC(C)(C)OC4)c(-c2ccccc2)c1C(=O)O	nan
	CHEMBL1310276	27621	8	None	-1	3	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	489	3	1	7	5.2	Cc1nc2c(sc3nc(N4CCOCC4)c4c(c32)CC(C)(C)OC4)c(-c2ccccc2)c1C(=O)O	nan
	CHEMBL267492	217503	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	162673931	189837	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794168	189837	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44577063	194879	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL498150	194879	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	24740653	95367	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	CHEMBL235556	95367	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	9842665	163585	12	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	162667953	189316	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787322	189316	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	162673931	189837	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794168	189837	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL267492	217503	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	101176453	189741	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4792986	189741	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	44410379	147981	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
	CHEMBL382833	147981	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
	24741624	145158	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
	CHEMBL377231	145158	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
	24741624	145158	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
	CHEMBL377231	145158	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
	10031074	83118	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
	CHEMBL205898	83118	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
	162667953	189316	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787322	189316	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	44246589	66035	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	13	2	5	5.3	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1C(C)C)N1C[C@@H](Cc2ccccc2)N(CCCC2CCCC2)C1=N	nan
	CHEMBL1703869	66035	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	13	2	5	5.3	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1C(C)C)N1C[C@@H](Cc2ccccc2)N(CCCC2CCCC2)C1=N	nan
	101176453	189741	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4792986	189741	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL267492	217503	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44410188	147158	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
	CHEMBL380854	147158	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
	44410385	146632	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
	CHEMBL379918	146632	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
	44433446	158743	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL396660	158743	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	3957801	66076	28	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	203	2	1	5	1.9	CCOC(=O)c1sc(S)nc1C	nan
	CHEMBL1705379	66076	28	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	203	2	1	5	1.9	CCOC(=O)c1sc(S)nc1C	nan
	24740655	95861	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	CHEMBL236521	95861	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	24740655	95861	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
	CHEMBL236521	95861	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
	44447804	162373	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL404503	162373	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	23635108	151741	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL391056	151741	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635108	151741	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL391056	151741	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	1190554	49697	12	None	-3	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	5	1	6	4.3	CCOC(=O)c1cnc2ccc(C)cc2c1Nc1ccc(N2CCOCC2)cc1	nan
	CHEMBL1503392	49697	12	None	-3	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	5	1	6	4.3	CCOC(=O)c1cnc2ccc(C)cc2c1Nc1ccc(N2CCOCC2)cc1	nan
	49778648	73764	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	429	8	1	7	3.7	c1ccc(COc2ccc(-c3cc4nc(NCCN5CCOCC5)ccn4n3)cc2)cc1	nan
	CHEMBL1868672	73764	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	429	8	1	7	3.7	c1ccc(COc2ccc(-c3cc4nc(NCCN5CCOCC5)ccn4n3)cc2)cc1	nan
	2713	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5353524	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5360566	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	88536661	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	9552079	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL1330113	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL790	212050	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	10855168	188685	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4779301	188685	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	10855168	188685	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4779301	188685	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	1326639	41657	10	None	-1	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	4	1	4	3.7	O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1	nan
	CHEMBL1431891	41657	10	None	-1	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	4	1	4	3.7	O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1	nan
	24180646	154961	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
	CHEMBL393576	154961	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
	24180646	154961	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393576	154961	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	44434568	95951	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL236650	95951	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL267492	217503	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44433262	152851	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL391914	152851	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	46902089	79698	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	5	2	7	4.3	CC(O)CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	CHEMBL2004734	79698	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	5	2	7	4.3	CC(O)CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	44202417	66533	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	643	8	4	6	5.7	COc1ccc(NC(=O)Nc2cccc3c2O[C@H](CN(C)C(=O)Nc2ccc(C(F)(F)F)cc2)[C@@H](C)CN([C@H](C)CO)C3=O)cc1	nan
	CHEMBL1725374	66533	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	643	8	4	6	5.7	COc1ccc(NC(=O)Nc2cccc3c2O[C@H](CN(C)C(=O)Nc2ccc(C(F)(F)F)cc2)[C@@H](C)CN([C@H](C)CO)C3=O)cc1	nan
	44447847	162211	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403749	162211	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	23635105	161758	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
	CHEMBL401250	161758	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
	23635105	161758	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL401250	161758	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
	17573520	62766	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1548086	62766	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1624390	62766	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL267492	217503	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	25211670	181039	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL454916	181039	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	44562460	196044	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL511826	196044	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	2998271	44620	9	None	1	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	5	2	5	4.1	CC(C)(C)c1cc(C(c2cccnc2)N2CCN(CCO)CC2)cc(C(C)(C)C)c1O	nan
	CHEMBL1458840	44620	9	None	1	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	5	2	5	4.1	CC(C)(C)c1cc(C(c2cccnc2)N2CCN(CCO)CC2)cc(C(C)(C)C)c1O	nan
	3216692	62422	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	CHEMBL1458479	62422	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	CHEMBL1621541	62422	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	44410207	168538	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
	CHEMBL413931	168538	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
	10481883	84110	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL208376	84110	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	10325306	148042	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL383117	148042	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	25058412	196219	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL513404	196219	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	44825857	73713	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	331	3	0	6	2.9	COc1ccc(CN2Cc3cnnn3-c3ccccc3C2C#N)cc1	nan
	CHEMBL1866397	73713	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	331	3	0	6	2.9	COc1ccc(CN2Cc3cnnn3-c3ccccc3C2C#N)cc1	nan
	135419062	34230	6	None	-1	2	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	431	5	1	7	4.5	N#Cc1c(O)nc(SCC(=O)c2ccc(Br)cc2)nc1-c1cccs1	nan
	CHEMBL1368444	34230	6	None	-1	2	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	431	5	1	7	4.5	N#Cc1c(O)nc(SCC(=O)c2ccc(Br)cc2)nc1-c1cccs1	nan
	2371253	35381	5	None	-5	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	458	7	1	6	4.5	O=C(COC(=O)c1ccccc1C(=O)c1ccc(Cl)c([N+](=O)[O-])c1)NC1CCCCCC1	nan
	CHEMBL1376861	35381	5	None	-5	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	458	7	1	6	4.5	O=C(COC(=O)c1ccccc1C(=O)c1ccc(Cl)c([N+](=O)[O-])c1)NC1CCCCCC1	nan
	44577060	194831	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL497746	194831	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	9842665	163585	12	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	23635237	98228	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
	CHEMBL240364	98228	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
	23635237	98228	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL240364	98228	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
	9842665	163585	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	44577092	185424	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467586	185424	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	9842665	163585	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	3573522	35529	16	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	374	3	1	5	4.6	CC1(C)CC(=O)C(C(C2=C(O)CC(C)(C)CC2=O)c2cccs2)C(=O)C1	nan
	CHEMBL1378309	35529	16	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	374	3	1	5	4.6	CC1(C)CC(=O)C(C(C2=C(O)CC(C)(C)CC2=O)c2cccs2)C(=O)C1	nan
	CHEMBL2370964	216746	0	None	-74	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2370964	216746	0	None	-74	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2370968	216750	0	None	-6	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	44577062	200153	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL525177	200153	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	4113455	79456	12	None	-1	2	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	463	4	1	6	4.1	C=CCn1/c(=N/C(=O)c2sc3ccccc3c2Cl)sc2cc(S(N)(=O)=O)ccc21	nan
	CHEMBL1996519	79456	12	None	-1	2	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	463	4	1	6	4.1	C=CCn1/c(=N/C(=O)c2sc3ccccc3c2Cl)sc2cc(S(N)(=O)=O)ccc21	nan
	44410175	175771	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL439158	175771	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
	44447773	102481	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL258245	102481	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	1846364	62866	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1589425	62866	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1625287	62866	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	162672837	189800	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793821	189800	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162672837	189800	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793821	189800	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	10369375	83993	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL207946	83993	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	44577090	185445	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467771	185445	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44433283	103235	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL262320	103235	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	23635235	173280	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL427860	173280	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635235	173280	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL427860	173280	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	44433297	159825	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397582	159825	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162676295	190232	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4798971	190232	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	101043845	197171	1	None	4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL5177536	197171	1	None	4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	9842665	163585	12	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	1002526	47889	11	None	-5	3	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	371	2	1	4	4.1	O=C(O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(Br)cc12	nan
	CHEMBL1488092	47889	11	None	-5	3	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	371	2	1	4	4.1	O=C(O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(Br)cc12	nan
	162676295	190232	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4798971	190232	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433264	96126	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL236940	96126	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673650	189832	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794121	189832	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162673650	189832	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794121	189832	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	759209	42745	10	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	259	1	0	3	3.5	Cc1c(Cl)sn(-c2ccc(Cl)cc2)c1=O	nan
	CHEMBL1442788	42745	10	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	259	1	0	3	3.5	Cc1c(Cl)sn(-c2ccc(Cl)cc2)c1=O	nan
	9842665	163585	12	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	1325	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	6440621	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	9898183	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL3422426	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	1325	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	6440621	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	9898183	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL3422426	10372	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	162668987	189369	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4788071	189369	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	2839884	52255	35	None	-	1	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	4	1	12	4.0	COC(=O)C1=C(C(=O)OC)SC2(S1)C(C(=O)OC)=C(C(=O)OC)SC1=C2c2cccc(C)c2NC1(C)C	nan
	CHEMBL1528149	52255	35	None	-	1	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	4	1	12	4.0	COC(=O)C1=C(C(=O)OC)SC2(S1)C(C(=O)OC)=C(C(=O)OC)SC1=C2c2cccc(C)c2NC1(C)C	nan
	4096875	66177	1	None	-	1	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	9	2	5	2.9	O=C(COC(=O)C(Cc1ccccc1)NC(=O)c1cccs1)NCc1ccccc1	nan
	CHEMBL1709842	66177	1	None	-	1	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	9	2	5	2.9	O=C(COC(=O)C(Cc1ccccc1)NC(=O)c1cccs1)NCc1ccccc1	nan
	162668987	189369	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4788071	189369	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44410041	148043	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
	CHEMBL383120	148043	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
	44577091	185446	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467772	185446	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	162675203	190040	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4796506	190040	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162675203	190040	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4796506	190040	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL2370968	216750	0	None	-6	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	162677173	190307	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799891	190307	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44562287	181027	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL454900	181027	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	162677173	190307	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799891	190307	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	23635107	98333	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240571	98333	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	44442981	159857	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397608	159857	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	23635107	98333	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240571	98333	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44577061	199420	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL521715	199420	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	44562440	185820	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL471340	185820	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
	1050448	48413	14	None	-4	2	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	385	4	0	4	5.6	COc1cc(-c2nc3ccc4ccccc4c3c3c2CCC3)cc(OC)c1OC	nan
	CHEMBL1491876	48413	14	None	-4	2	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	385	4	0	4	5.6	COc1cc(-c2nc3ccc4ccccc4c3c3c2CCC3)cc(OC)c1OC	nan
	24180593	155222	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393788	155222	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	216239	30567	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	CHEMBL1200485	30567	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	CHEMBL1336	30567	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	9983075	84083	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL208268	84083	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
	44433279	158488	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL396433	158488	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673640	189761	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793346	189761	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44443035	161196	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	CHEMBL398929	161196	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	44433272	154490	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393204	154490	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673640	189761	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793346	189761	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44577089	185526	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL468579	185526	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44577064	194696	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL496710	194696	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	44433294	159822	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397580	159822	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	24740419	154973	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
	CHEMBL393584	154973	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
	CHEMBL267492	217503	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	162643518	188490	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776915	188490	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162643518	188490	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776915	188490	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	1482612	32022	16	None	-	1	Human	5.3	pIC50	=	5.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	407	3	1	5	5.0	O=C(O)c1cnn(-c2nc(-c3ccc(Cl)c(Cl)c3)cs2)c1C(F)(F)F	nan
	CHEMBL1348506	32022	16	None	-	1	Human	5.3	pIC50	=	5.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	407	3	1	5	5.0	O=C(O)c1cnn(-c2nc(-c3ccc(Cl)c(Cl)c3)cs2)c1C(F)(F)F	nan
	23661656	175823	0	None	7	2	Human	6.3	pIC50	=	6.3	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL439560	175823	0	None	7	2	Human	6.3	pIC50	=	6.3	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
	44433298	159826	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397583	159826	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162672763	189903	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794990	189903	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44447777	162194	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403675	162194	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	162664942	188972	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4782808	188972	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162664942	188972	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4782808	188972	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433285	95391	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL235640	95391	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162672763	189903	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794990	189903	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	10075878	82766	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL205461	82766	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	44447250	101502	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
	CHEMBL253028	101502	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
	1343565	45635	9	None	-	1	Human	4.3	pIC50	=	4.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	2	6	3.8	Cc1ccc(-n2nc3ccc(NC(=S)NC(=O)/C=C/c4ccco4)cc3n2)cc1	nan
	CHEMBL1467018	45635	9	None	-	1	Human	4.3	pIC50	=	4.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	2	6	3.8	Cc1ccc(-n2nc3ccc(NC(=S)NC(=O)/C=C/c4ccco4)cc3n2)cc1	nan
	16046215	86864	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
	CHEMBL213122	86864	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
	44455922	161915	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL402075	161915	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
	9842665	163585	12	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	101043845	197171	1	None	4	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL5177536	197171	1	None	4	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	16046215	86864	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
	CHEMBL213122	86864	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
	10414731	83323	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL206141	83323	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
	874744	48179	8	None	-	1	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	269	3	1	2	3.9	C=C1CCc2c([nH]c3ccc(OCC(C)C)cc23)C1=O	nan
	CHEMBL1490308	48179	8	None	-	1	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	269	3	1	2	3.9	C=C1CCc2c([nH]c3ccc(OCC(C)C)cc23)C1=O	nan
	9842665	163585	12	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	28777	52788	80	None	-	1	Human	4.2	pIC50	=	4.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	261	2	0	3	3.3	O=C1c2ccccc2C(=O)N1SC1CCCCC1	nan
	CHEMBL1532794	52788	80	None	-	1	Human	4.2	pIC50	=	4.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	261	2	0	3	3.3	O=C1c2ccccc2C(=O)N1SC1CCCCC1	nan
	448949	127570	89	None	-5	3	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	355	2	3	3	5.2	O=Nc1c(-c2c(O)[nH]c3cc(Br)ccc23)[nH]c2ccccc12	nan
	CHEMBL355496	127570	89	None	-5	3	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	355	2	3	3	5.2	O=Nc1c(-c2c(O)[nH]c3cc(Br)ccc23)[nH]c2ccccc12	nan
	44456219	162217	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL403806	162217	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	162643092	188503	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4777048	188503	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44447785	101852	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL255313	101852	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	44433439	96699	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL237976	96699	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	162643092	188503	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4777048	188503	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44410046	82726	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
	CHEMBL205214	82726	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
	44562414	183596	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL460942	183596	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	162665567	189128	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784635	189128	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	44410378	83401	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
	CHEMBL206367	83401	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
	23635106	98332	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240568	98332	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	23635106	98332	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240568	98332	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	162665567	189128	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784635	189128	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	11756904	83361	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
	CHEMBL206316	83361	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
	44447221	101444	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
	CHEMBL252584	101444	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
	44410040	83293	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL205996	83293	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	9842665	163585	12	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	163585	12	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	44143139	66542	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	673	13	2	5	6.4	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@@H]1Cc1ccccc1)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	CHEMBL1725591	66542	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	673	13	2	5	6.4	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@@H]1Cc1ccccc1)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	44447780	101819	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL255100	101819	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	44825858	74228	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	315	2	0	5	3.2	Cc1ccccc1CN1Cc2cnnn2-c2ccccc2C1C#N	nan
	CHEMBL1891068	74228	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	315	2	0	5	3.2	Cc1ccccc1CN1Cc2cnnn2-c2ccccc2C1C#N	nan
	3617229	51276	7	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	394	4	2	4	5.4	O=C(Nc1ccccc1)OC1CCC2CC1CCC2OC(=O)Nc1ccccc1	nan
	CHEMBL1519347	51276	7	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	394	4	2	4	5.4	O=C(Nc1ccccc1)OC1CCC2CC1CCC2OC(=O)Nc1ccccc1	nan
	44577055	200075	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL524060	200075	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	1336753	36937	14	None	-7	4	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	1	6	3.9	O=[N+]([O-])c1cc(S(=O)(=O)C(F)(F)F)ccc1Sc1nc2ccccc2[nH]1	nan
	CHEMBL1390139	36937	14	None	-7	4	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	1	6	3.9	O=[N+]([O-])c1cc(S(=O)(=O)C(F)(F)F)ccc1Sc1nc2ccccc2[nH]1	nan
	44246581	37445	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	639	14	2	5	6.4	CCC[C@@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1CC(C)C)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	CHEMBL1394750	37445	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	639	14	2	5	6.4	CCC[C@@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1CC(C)C)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	162644475	188584	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4778074	188584	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	162644475	188584	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4778074	188584	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	162677133	190336	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4800268	190336	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162677133	190336	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4800268	190336	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	42628546	66620	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	382	8	0	2	5.6	CCCCCCCN(c1ccccc1)[C@H]1C[C@@H]2CCN3C(=O)CCC[C@H](C1)[C@H]23	nan
	CHEMBL1728670	66620	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	382	8	0	2	5.6	CCCCCCCN(c1ccccc1)[C@H]1C[C@@H]2CCN3C(=O)CCC[C@H](C1)[C@H]23	nan
	CHEMBL267492	217503	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44433299	159827	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397584	159827	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	5291838	49463	10	None	3	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	287	2	0	4	3.9	CC1=NOC(=O)/C1=C/c1ccc(-c2ccc(Cl)cc2)o1	nan
	CHEMBL1501376	49463	10	None	3	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	287	2	0	4	3.9	CC1=NOC(=O)/C1=C/c1ccc(-c2ccc(Cl)cc2)o1	nan
	2575495	52557	6	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	534	9	2	6	4.1	O=C(COC(=O)CNS(=O)(=O)c1cccc(Br)c1)Nc1ccccc1Sc1ccccc1	nan
	CHEMBL1530780	52557	6	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	534	9	2	6	4.1	O=C(COC(=O)CNS(=O)(=O)c1cccc(Br)c1)Nc1ccccc1Sc1ccccc1	nan
	1335691	32321	5	None	1	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	4	1	5	3.2	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1Cl	nan
	CHEMBL1351081	32321	5	None	1	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	4	1	5	3.2	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1Cl	nan
	10049407	84105	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
	CHEMBL208366	84105	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
	1190175	26360	9	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	449	7	1	8	4.2	CCOC(=O)c1ccc2ncc(C(=O)OCC)c(Nc3ccc(N4CCOCC4)cc3)c2c1	nan
	CHEMBL1300063	26360	9	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	449	7	1	8	4.2	CCOC(=O)c1ccc2ncc(C(=O)OCC)c(Nc3ccc(N4CCOCC4)cc3)c2c1	nan
	23635236	98376	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240780	98376	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
	23635236	98376	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240780	98376	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	362664	66949	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	CHEMBL1699592	66949	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	CHEMBL1739768	66949	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	23635109	98334	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL240572	98334	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635109	98334	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL240572	98334	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	44447804	162373	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL404503	162373	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	24180592	103788	0	None	-1	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
	CHEMBL266647	103788	0	None	-1	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
	44601668	65905	0	None	2	2	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	428	4	1	3	5.6	O=S(=O)(/C(=C\c1ccc(C(F)(F)F)cc1)c1nc2ccccc2[nH]1)c1ccccc1	nan
	CHEMBL1698464	65905	0	None	2	2	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	428	4	1	3	5.6	O=S(=O)(/C(=C\c1ccc(C(F)(F)F)cc1)c1nc2ccccc2[nH]1)c1ccccc1	nan
	44433293	151701	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL391028	151701	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	44447851	101711	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL254364	101711	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	44410176	82799	7	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
	CHEMBL205594	82799	7	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
	162675582	190239	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799036	190239	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162675582	190239	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799036	190239	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433271	96314	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
	CHEMBL237365	96314	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
	1472220	48669	11	None	-4	3	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	418	6	1	4	4.3	COc1ccc(NC(=O)/C(Cl)=C(/Cl)[S+]([O-])Cc2ccc(Cl)cc2)cn1	nan
	CHEMBL1494120	48669	11	None	-4	3	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	418	6	1	4	4.3	COc1ccc(NC(=O)/C(Cl)=C(/Cl)[S+]([O-])Cc2ccc(Cl)cc2)cn1	nan
	CHEMBL428801	220251	0	None	-21	5	Human	9.7	pKd	=	9.7	Functional	Evaluated for partial agonistic activity at cloned mammalian Melanocortin 4 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	145953129	169219	0	None	-	0	Mouse	9.6	pKd	=	9.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1001	16	13	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4166449	169219	0	None	-	0	Mouse	9.6	pKd	=	9.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1001	16	13	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145957551	169043	0	None	-	1	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1015	17	13	11	-1.5	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4163787	169043	0	None	-	1	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1015	17	13	11	-1.5	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145960041	169065	0	None	-	0	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	945	14	11	11	-1.8	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4164111	169065	0	None	-	0	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	945	14	11	11	-1.8	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	127035019	143214	0	None	-	1	Mouse	9.3	pKd	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	143214	0	None	-	1	Mouse	9.3	pKd	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL266417	217462	0	None	-50	6	Human	9.3	pKd	=	9.3	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	145952883	169194	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	973	15	11	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4166050	169194	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	973	15	11	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145951686	169735	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	979	13	11	11	-1.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4174761	169735	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	979	13	11	11	-1.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL2096742	215985	0	None	-1	6	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm070461w
	137655051	165745	0	None	-	0	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4096081	165745	0	None	-	0	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	127035019	143214	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	143214	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	145956526	168971	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	929	13	10	10	-0.8	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4162603	168971	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	929	13	10	10	-0.8	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145958585	169118	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	931	13	11	11	-2.2	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4164846	169118	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	931	13	11	11	-2.2	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145954663	169436	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	985	15	12	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4169872	169436	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	985	15	12	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145950765	169612	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	964	12	11	11	-2.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4172753	169612	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	964	12	11	11	-2.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	145951839	169654	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4173301	169654	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	162650385	186850	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4747952	186850	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	145957356	168767	0	None	-	0	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1035	15	13	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4159229	168767	0	None	-	0	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1035	15	13	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	145954673	169450	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	915	12	10	10	-1.2	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4170160	169450	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	915	12	10	10	-1.2	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145951083	169755	0	None	-	0	Mouse	8.9	pKd	=	8.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1033	15	12	10	-0.4	C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4175108	169755	0	None	-	0	Mouse	8.9	pKd	=	8.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1033	15	12	10	-0.4	C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	145952946	169264	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	999	16	12	10	-0.5	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4167239	169264	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	999	16	12	10	-0.5	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145949639	169536	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1049	16	13	11	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4171666	169536	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1049	16	13	11	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	132938008	166292	0	None	3	5	Mouse	8.7	pKd	=	8.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4102048	166292	0	None	3	5	Mouse	8.7	pKd	=	8.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	122184635	129212	0	None	-56	4	Human	8.0	pKd	=	8	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600916	129212	0	None	-56	4	Human	8.0	pKd	=	8	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	127046262	146598	0	None	23	3	Mouse	8.0	pKd	=	8.0	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798912	146598	0	None	23	3	Mouse	8.0	pKd	=	8.0	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	132180597	162950	0	None	-117	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4063911	162950	0	None	-117	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155542149	179871	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	740	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4520119	179871	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	740	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155544214	180110	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	797	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4526652	180110	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	797	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155563222	182070	0	None	-524	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4572994	182070	0	None	-524	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137662060	165984	0	None	-	1	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	991	13	10	10	-0.2	C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4098651	165984	0	None	-	1	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	991	13	10	10	-0.2	C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659091	166119	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4100160	166119	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137657151	166335	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4102613	166335	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	155546131	180309	0	None	2	5	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4531291	180309	0	None	2	5	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162664463	188969	0	None	-	3	Mouse	5.0	pKd	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4782762	188969	0	None	-	3	Mouse	5.0	pKd	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL2370694	216690	0	None	-	1	Mouse	7.0	pKd	=	7.0	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	6918814	133835	1	None	-	0	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	CHEMBL365597	133835	1	None	-	0	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	137642804	165150	0	None	-	1	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4089759	165150	0	None	-	1	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	132180653	181838	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567961	181838	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137641768	164885	0	None	-	0	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	13	9	9	1.1	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4086679	164885	0	None	-	0	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	13	9	9	1.1	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	162673830	189938	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4795352	189938	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	137635892	162684	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4060738	162684	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137633477	163374	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4068777	163374	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137643799	165217	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4090448	165217	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155556047	181276	0	None	-199	4	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4554828	181276	0	None	-199	4	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137654977	165585	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	11	9	9	0.6	CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4094419	165585	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	11	9	9	0.6	CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155536962	179016	0	None	10	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4474215	179016	0	None	10	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162672755	189869	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	189869	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	164610489	191334	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	600	10	4	4	5.8	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4848322	191334	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	600	10	4	4	5.8	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL2370695	216691	0	None	-1	2	Mouse	5.9	pKd	=	5.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	127046262	146598	0	None	-	3	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798912	146598	0	None	-	3	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL2370696	216692	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	CHEMBL103817	215238	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	127047336	146576	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798768	146576	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	155548853	180588	0	None	-6	5	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4538274	180588	0	None	-6	5	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	132180598	164628	0	None	-25	4	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4083717	164628	0	None	-25	4	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL407346	219435	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	137632506	163303	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1049	12	10	9	1.6	C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4067947	163303	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1049	12	10	9	1.6	C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	145955736	169332	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1331	22	17	17	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4168324	169332	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1331	22	17	17	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	155555217	181116	0	None	-812	4	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550976	181116	0	None	-812	4	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162649653	186879	0	None	-	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4748317	186879	0	None	-	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL2096710	215984	0	None	-53	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonistic activity against mouse Melanocortin 4 ReceptorAntagonistic activity against mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049620r
	44310372	165360	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932915	165360	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL409190	165360	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	155536962	179016	0	None	-10	3	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4474215	179016	0	None	-10	3	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155566718	182695	0	None	-3	2	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4587214	182695	0	None	-3	2	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137657385	166545	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	867	21	11	7	0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4105142	166545	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	867	21	11	7	0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164609130	191206	0	None	-	3	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	595	10	4	4	5.1	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4846261	191206	0	None	-	3	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	595	10	4	4	5.1	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	164621263	192261	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	598	11	3	3	7.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1	10.1021/acs.jmedchem.0c02041
	CHEMBL4862172	192261	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	598	11	3	3	7.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1	10.1021/acs.jmedchem.0c02041
	164624627	192658	0	None	-3	4	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868223	192658	0	None	-3	4	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	164627764	193343	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	603	11	4	4	4.8	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4878201	193343	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	603	11	4	4	4.8	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	137653029	165494	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	977	12	10	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4093379	165494	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	977	12	10	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137639030	163724	0	None	-	0	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	963	11	10	10	-0.7	C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4072662	163724	0	None	-	0	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	963	11	10	10	-0.7	C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659851	166216	0	None	-	0	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	949	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4101128	166216	0	None	-	0	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	949	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137654791	165697	0	None	-	0	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1053	14	10	10	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4095539	165697	0	None	-	0	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1053	14	10	10	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659513	166029	0	None	-	1	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4099096	166029	0	None	-	1	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155553683	180962	0	None	-295	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4547556	180962	0	None	-295	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155567399	182745	0	None	-501	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4588429	182745	0	None	-501	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	137640475	163866	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	870	16	7	6	2.9	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4074368	163866	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	870	16	7	6	2.9	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137649203	164287	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	894	18	8	8	3.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079721	164287	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	894	18	8	8	3.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137653704	165412	0	None	-2	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4092424	165412	0	None	-2	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137658359	166350	0	None	-8	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4102774	166350	0	None	-8	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	162671821	189682	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4792291	189682	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	132938008	166292	0	None	3	5	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4102048	166292	0	None	3	5	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	145951904	169718	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	957	14	10	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4174361	169718	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	957	14	10	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145973163	169863	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1007	14	11	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4176668	169863	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1007	14	11	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	137638391	163637	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4071633	163637	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127047336	146576	0	None	33	4	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798768	146576	0	None	33	4	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	137644456	165092	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1010	12	9	9	1.1	C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4089149	165092	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1010	12	9	9	1.1	C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155544852	181718	0	None	-3	5	Human	7.6	pKd	=	7.6	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4565367	181718	0	None	-3	5	Human	7.6	pKd	=	7.6	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155543031	179960	0	None	-50	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4522298	179960	0	None	-50	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155564058	182113	0	None	-794	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4574056	182113	0	None	-794	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	162653604	187274	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4753150	187274	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O	10.1021/acsmedchemlett.9b00641
	137639815	163581	0	None	-1	4	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4071063	163581	0	None	-1	4	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646086	164673	0	None	-	1	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	908	19	8	6	3.8	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4084136	164673	0	None	-	1	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	908	19	8	6	3.8	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646802	164730	0	None	-	2	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4084671	164730	0	None	-	2	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	155555182	181100	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	778	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550582	181100	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	778	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162670795	189605	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4791112	189605	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	137635794	163030	0	None	-	1	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	858	19	8	6	2.7	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4064881	163030	0	None	-	1	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	858	19	8	6	2.7	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137642664	164859	0	None	-	3	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	772	18	9	7	-0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4086346	164859	0	None	-	3	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	772	18	9	7	-0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164623182	192398	0	None	-	2	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	607	11	4	4	5.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4864094	192398	0	None	-	2	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	607	11	4	4	5.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	145959370	168786	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	959	14	11	11	-2.3	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4159541	168786	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	959	14	11	11	-2.3	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	44310103	173426	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	77231882	173426	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL428134	173426	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	162645080	186229	0	None	-	1	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	976	12	9	10	-0.9	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4740561	186229	0	None	-	1	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	976	12	9	10	-0.9	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	162649541	186834	0	None	-	0	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	963	12	9	10	-0.8	C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4747778	186834	0	None	-	0	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	963	12	9	10	-0.8	C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	155561116	181752	0	None	-7	5	Human	7.5	pKd	=	7.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4566163	181752	0	None	-7	5	Human	7.5	pKd	=	7.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162662360	188250	0	None	-	2	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4764556	188250	0	None	-	2	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	155544852	181718	0	None	3	5	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4565367	181718	0	None	3	5	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL2373991	217160	0	None	14	3	Mouse	7.5	pKd	=	7.5	Functional	Antagonistic activity against mouse Melanocortin 4 ReceptorAntagonistic activity against mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/jm049620r
	155532232	178484	0	None	-7	2	Human	6.5	pKd	=	6.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4466724	178484	0	None	-7	2	Human	6.5	pKd	=	6.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155562237	182488	0	None	-1548	4	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4582276	182488	0	None	-1548	4	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162654633	187423	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4754987	187423	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162672755	189869	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	189869	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	164624386	192977	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	593	10	4	4	5.0	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4872932	192977	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	593	10	4	4	5.0	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	137634306	163101	0	None	-	2	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4065669	163101	0	None	-	2	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164625589	192520	0	None	-	1	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	612	11	3	3	7.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4866151	192520	0	None	-	1	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	612	11	3	3	7.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	155546131	180309	0	None	-2	5	Human	6.4	pKd	=	6.4	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4531291	180309	0	None	-2	5	Human	6.4	pKd	=	6.4	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	132180599	163672	0	None	-1	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4072129	163672	0	None	-1	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137649368	164185	0	None	-6	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4078495	164185	0	None	-6	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137653916	165359	0	None	-3	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4091894	165359	0	None	-3	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137657607	166415	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4103567	166415	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155556466	181195	0	None	-2238	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4552764	181195	0	None	-2238	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155563055	182074	0	None	-75	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4573041	182074	0	None	-75	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162666503	189009	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4783292	189009	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	162662213	188275	0	None	-	3	Mouse	5.4	pKd	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4764827	188275	0	None	-	3	Mouse	5.4	pKd	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	127047624	146674	0	None	31	3	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799408	146674	0	None	31	3	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	137631920	163215	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	12	9	9	0.9	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4066929	163215	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	12	9	9	0.9	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	137650523	164133	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	933	10	9	9	-0.1	C[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4077783	164133	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	933	10	9	9	-0.1	C[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL2370695	216691	0	None	-1	2	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	CHEMBL264190	217387	1	None	-2	8	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137656661	166504	0	None	-	0	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1000	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4104582	166504	0	None	-	0	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1000	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL454736	220776	0	None	-	2	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137645343	164575	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	9	9	0.3	CCC1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4083137	164575	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	9	9	0.3	CCC1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155561116	181752	0	None	7	5	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4566163	181752	0	None	7	5	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137651071	164246	0	None	-16	4	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079298	164246	0	None	-16	4	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155566718	182695	0	None	3	2	Mouse	5.3	pKd	=	5.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4587214	182695	0	None	3	2	Mouse	5.3	pKd	=	5.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155536388	178919	0	None	-	0	Human	7.3	pKd	=	7.3	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1660	36	16	19	-4.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4473100	178919	0	None	-	0	Human	7.3	pKd	=	7.3	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1660	36	16	19	-4.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3577981	218528	1	None	-1	5	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	137649684	163917	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	992	13	11	11	-2.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4075125	163917	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	992	13	11	11	-2.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL3577981	218528	1	None	-1	5	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137632217	163081	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	900	10	10	10	-2.4	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4065443	163081	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	900	10	10	10	-2.4	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155548853	180588	0	None	6	5	Mouse	7.2	pKd	=	7.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4538274	180588	0	None	6	5	Mouse	7.2	pKd	=	7.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137640715	163782	0	None	-	3	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4073316	163782	0	None	-	3	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155550083	180693	0	None	-134	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4540411	180693	0	None	-134	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155558348	181815	0	None	-61	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567480	181815	0	None	-61	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155568641	182876	0	None	-660	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4591394	182876	0	None	-660	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	137636060	163010	0	None	-	2	Mouse	5.2	pKd	=	5.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4064728	163010	0	None	-	2	Mouse	5.2	pKd	=	5.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137642489	164972	0	None	-	0	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1019	14	10	10	-0.2	CC(C)C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4087835	164972	0	None	-	0	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1019	14	10	10	-0.2	CC(C)C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127047624	146674	0	None	-	3	Human	8.1	pKd	=	8.1	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799408	146674	0	None	-	3	Human	8.1	pKd	=	8.1	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	137654466	165510	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1034	16	11	11	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4093505	165510	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1034	16	11	11	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155539948	179665	0	None	-131	4	Mouse	7.1	pKd	=	7.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4515666	179665	0	None	-131	4	Mouse	7.1	pKd	=	7.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162647356	186459	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-1.2	CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4743564	186459	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-1.2	CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O	10.1021/acsmedchemlett.9b00641
	137632948	163361	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4068643	163361	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137651782	164272	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079580	164272	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646614	164317	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4080138	164317	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155547310	180390	0	None	-	3	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	750	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4533593	180390	0	None	-	3	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	750	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155565321	182355	0	None	-100	4	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4579448	182355	0	None	-100	4	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	137631703	163182	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	12	10	10	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4066514	163182	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	12	10	10	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155532232	178484	0	None	7	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4466724	178484	0	None	7	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL103817	215238	0	None	2	4	Mouse	8.1	pKd	=	8.1	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	137640194	163738	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1043	14	11	11	-1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4072797	163738	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1043	14	11	11	-1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127035019	143214	0	None	-	1	Mouse	9.3	pKi	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	143214	0	None	-	1	Mouse	9.3	pKi	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	137655051	165745	0	None	-	0	Human	9.1	pKi	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4096081	165745	0	None	-	0	Human	9.1	pKi	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	127035019	143214	0	None	-	1	Mouse	9.1	pKi	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	143214	0	None	-	1	Mouse	9.1	pKi	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	162664463	188969	0	None	-	3	Mouse	5.0	pKi	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4782762	188969	0	None	-	3	Mouse	5.0	pKi	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162673830	189938	0	None	-	3	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4795352	189938	0	None	-	3	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	137642804	165150	0	None	-	1	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4089759	165150	0	None	-	1	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	132180598	164628	0	None	-25	4	Mouse	7.8	pKi	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4083717	164628	0	None	-25	4	Mouse	7.8	pKi	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	2804382	107121	3	None	-	0	Mouse	4.8	pKi	=	4.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	318	4	1	3	4.0	Fc1cccc(F)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL289532	107121	3	None	-	0	Mouse	4.8	pKi	=	4.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	318	4	1	3	4.0	Fc1cccc(F)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	162649653	186879	0	None	-	3	Mouse	6.8	pKi	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4748317	186879	0	None	-	3	Mouse	6.8	pKi	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	9842665	163585	12	None	-	1	Mouse	6.8	pKi	=	6.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL40711	163585	12	None	-	1	Mouse	6.8	pKi	=	6.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL454736	220776	0	None	-	2	Mouse	7.7	pKi	=	7.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	162671821	189682	0	None	-	3	Mouse	5.7	pKi	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4792291	189682	0	None	-	3	Mouse	5.7	pKi	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	9864301	161956	0	None	-	0	Mouse	6.7	pKi	=	6.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	372	5	1	3	4.0	COc1ccc(Br)cc1CCc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL40233	161956	0	None	-	0	Mouse	6.7	pKi	=	6.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	372	5	1	3	4.0	COc1ccc(Br)cc1CCc1ccccc1C1=NCCCN1	10.1021/jm034244g
	2806083	106935	3	None	-	0	Mouse	5.7	pKi	=	5.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	356	4	1	4	5.1	Clc1cc(CSc2ccccc2C2=NCCCN2)c(Cl)s1	10.1021/jm034244g
	CHEMBL287895	106935	3	None	-	0	Mouse	5.7	pKi	=	5.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	356	4	1	4	5.1	Clc1cc(CSc2ccccc2C2=NCCCN2)c(Cl)s1	10.1021/jm034244g
	162670795	189605	0	None	-	3	Mouse	6.6	pKi	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4791112	189605	0	None	-	3	Mouse	6.6	pKi	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	605683	164809	3	None	-	0	Mouse	5.6	pKi	=	5.6	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	334	4	1	3	4.5	Fc1cccc(Cl)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL40857	164809	3	None	-	0	Mouse	5.6	pKi	=	5.6	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	334	4	1	3	4.5	Fc1cccc(Cl)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	162654633	187423	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4754987	187423	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162672755	189869	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	189869	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	11245316	175289	0	None	-	0	Mouse	7.4	pKi	=	7.4	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	358	5	1	3	3.6	COc1ccc(Br)cc1CCc1ccccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL435368	175289	0	None	-	0	Mouse	7.4	pKi	=	7.4	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	358	5	1	3	3.6	COc1ccc(Br)cc1CCc1ccccc1C1=NCCN1	10.1021/jm034244g
	162662213	188275	0	None	-	3	Mouse	5.4	pKi	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4764827	188275	0	None	-	3	Mouse	5.4	pKi	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162666503	189009	0	None	-	3	Mouse	6.4	pKi	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4783292	189009	0	None	-	3	Mouse	6.4	pKi	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	10293816	168955	0	None	-	0	Mouse	7.2	pKi	=	7.2	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	390	5	1	4	4.5	COc1ccc(Br)cc1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL416244	168955	0	None	-	0	Mouse	7.2	pKi	=	7.2	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	390	5	1	4	4.5	COc1ccc(Br)cc1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	129627786	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	1330	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16129617	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16129674	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16133751	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16133802	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16162116	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	3767	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	4516	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	60210072	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	6965	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	CHEMBL2103784	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	DB01284	7068	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	131839615	219415	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	16133835	219415	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	CHEMBL407070	219415	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	1339	9243	0	None	-	1	Human	10.0	pIC50	=	10	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11606131
	1338	10579	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	9938402	10579	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	CHEMBL339053	10579	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	1341	9850	0	None	-251	3	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12431055
	1337	10197	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	6918851	10197	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	CHEMBL364346	10197	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	1335	7103	0	None	39	3	Human	9.3	pIC50	None	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9299416

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Similar- ity	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
		1046	209431	116	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	123	1	1	3	-0.4	NC(=O)c1cnccn1	10.1038/s41467-023-40064-9
		CHEMBL614	209431	116	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	123	1	1	3	-0.4	NC(=O)c1cnccn1	10.1038/s41467-023-40064-9
		68617	212306	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		CHEMBL1709	212306	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		CHEMBL809	212306	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		1016	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		2561	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		2733526	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		5384	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL83	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		DB00675	10519	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		4212	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		CHEMBL1417019	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		CHEMBL58	205458	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		2351	11072	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		CHEMBL1008	11072	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		CHEMBL1257078	11072	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		1155	8410	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		3343	8410	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		557	8410	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		CHEMBL32800	8410	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		DB01288	8410	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		2162	48288	100	None	-	6	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
		CHEMBL1491	48288	100	None	-	6	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
		1212	8443	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		204	8443	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		3372	8443	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		CHEMBL726	8443	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		DB00623	8443	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		1222	8445	49	None	-	32	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		3396	8445	49	None	-	32	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		85	8445	49	None	-	32	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL46516	8445	49	None	-	32	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		DB04842	8445	49	None	-	32	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		2726	7706	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		621	7706	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		83	7706	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		CHEMBL71	7706	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		DB00477	7706	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		16362	9899	71	None	-	29	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		2172	9899	71	None	-	29	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		90	9899	71	None	-	29	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		CHEMBL1423	9899	71	None	-	29	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		DB01100	9899	71	None	-	29	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		25077405	9492	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		3902	9492	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		CHEMBL1201309	9492	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		DB00666	9492	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		180	7189	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		200	7189	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		2160	7189	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		CHEMBL629	7189	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		DB00321	7189	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		5328940	106992	107	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
		CHEMBL288441	106992	107	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
		202	8290	77	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		60835	8290	77	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		972	8290	77	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		CHEMBL1175	8290	77	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		DB00476	8290	77	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		11626560	207716	94	None	-	0	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
		CHEMBL601719	207716	94	None	-	0	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
		1353	8692	93	None	-	85	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		3559	8692	93	None	-	85	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		86	8692	93	None	-	85	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		CHEMBL54	8692	93	None	-	85	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		DB00502	8692	93	None	-	85	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		1427	8794	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		357	8794	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		3696	8794	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		CHEMBL11	8794	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		DB00458	8794	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		176	7186	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		2157	7186	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		2566	7186	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		CHEMBL633	7186	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		DB01118	7186	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		4046	9261	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		4252	9261	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		CHEMBL416956	9261	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		DB00358	9261	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		3676	212049	101	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	234	5	1	2	2.6	CCN(CC)CC(=O)Nc1c(C)cccc1C	10.1038/s41467-023-40064-9
		CHEMBL79	212049	101	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	234	5	1	2	2.6	CCN(CC)CC(=O)Nc1c(C)cccc1C	10.1038/s41467-023-40064-9
		1056	10144	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		2405	10144	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		77999	10144	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		CHEMBL121	10144	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		DB00412	10144	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		4046	9261	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		4252	9261	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		CHEMBL416956	9261	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		DB00358	9261	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		5090	22333	106	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	10.1038/s41467-023-40064-9
		CHEMBL122	22333	106	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	10.1038/s41467-023-40064-9
		4236	34869	66	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	273	5	1	2	2.0	NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL1373	34869	66	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	273	5	1	2	2.0	NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		2286	9957	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		4927	9957	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		7282	9957	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		CHEMBL643	9957	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		DB01069	9957	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		3899	214553	119	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	270	2	1	3	3.3	Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1	10.1038/s41467-023-40064-9
		CHEMBL960	214553	119	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	270	2	1	3	3.3	Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1	10.1038/s41467-023-40064-9
		16220172	79818	95	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	392	2	3	3	5.1	CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O	10.1038/s41467-023-40064-9
		CHEMBL2010601	79818	95	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	392	2	3	3	5.1	CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O	10.1038/s41467-023-40064-9
		2713	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		5353524	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		5360566	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		88536661	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		9552079	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		CHEMBL1330113	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		CHEMBL790	212050	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		6436173	61890	45	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	785	2	5	13	6.2	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
		CHEMBL1617	61890	45	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	785	2	5	13	6.2	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
		104850	10103	96	None	-	6	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		4150	10103	96	None	-	6	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		743	10103	96	None	-	6	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		CHEMBL111	10103	96	None	-	6	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		DB06155	10103	96	None	-	6	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		124087	8171	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		7157	8171	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		814	8171	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		CHEMBL1172	8171	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		DB00967	8171	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		2200	26975	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		CHEMBL1256819	26975	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		CHEMBL1305	26975	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		26987	7736	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		6063	7736	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		671	7736	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		CHEMBL1626	7736	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		DB00283	7736	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		2585	7590	103	None	-	22	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		522	7590	103	None	-	22	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		551	7590	103	None	-	22	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		CHEMBL723	7590	103	None	-	22	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		DB01136	7590	103	None	-	22	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		2812	11551	101	None	-	34	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
		CHEMBL104	11551	101	None	-	34	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
		2398	7741	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		2801	7741	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		701	7741	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		CHEMBL415	7741	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		DB01242	7741	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		54675785	100988	42	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	442	2	6	9	-0.4	C=C1c2cccc(O)c2C(=O)C2=C(O)[C@]3(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]3[C@@H](O)[C@H]12	10.1038/s41467-023-40064-9
		CHEMBL249837	100988	42	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	442	2	6	9	-0.4	C=C1c2cccc(O)c2C(=O)C2=C(O)[C@]3(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]3[C@@H](O)[C@H]12	10.1038/s41467-023-40064-9
		10096344	96369	85	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
		CHEMBL237500	96369	85	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
		135409453	10545	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		226	10545	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		CHEMBL76370	10545	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		9801	98360	35	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL24072	98360	35	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		2600	10551	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		2608	10551	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		5405	10551	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		CHEMBL17157	10551	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		DB00342	10551	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		8550	21196	57	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	578	7	1	9	4.2	COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC	10.1038/s41467-023-40064-9
		CHEMBL1200515	21196	57	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	578	7	1	9	4.2	COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC	10.1038/s41467-023-40064-9
		2274	9947	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		4917	9947	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		7279	9947	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		CHEMBL728	9947	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		DB00433	9947	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		214	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		2740	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		5566	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		66064	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		CHEMBL422	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		DB00831	10632	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		100	10577	58	None	-	54	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		2637	10577	58	None	-	54	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		5452	10577	58	None	-	54	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		CHEMBL479	10577	58	None	-	54	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		DB00679	10577	58	None	-	54	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		1324	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		16154396	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		16197727	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		44285019	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		57514683	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		91898441	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		CHEMBL441738	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		DB04931	7090	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		1323	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		92432	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL430239	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		1323	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		92432	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL430239	9465	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		1323	9465	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		92432	9465	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		CHEMBL430239	9465	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		1323	9465	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		92432	9465	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		CHEMBL430239	9465	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		44327392	148641	0	None	-	0	Mouse	10.1	pEC50	=	10.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	1025	21	12	12	-0.6	CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0104872
		CHEMBL386583	148641	0	None	-	0	Mouse	10.1	pEC50	=	10.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	1025	21	12	12	-0.6	CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0104872
		CHEMBL2369959	216519	0	None	-	0	Mouse	9.9	pEC50	=	9.9	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		1324	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		16154396	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		16197727	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		44285019	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		57514683	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		91898441	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL441738	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		DB04931	7090	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL217305	216152	0	None	-	0	Human	9.8	pEC50	=	9.8	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1016/s0960-894x(03)00412-8
		CHEMBL415165	219955	0	None	-3	5	Human	9.7	pEC50	=	9.7	Binding	Effective concentration against human melanocortin-4 receptor Effective concentration against human melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm0501432
		1324	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16154396	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16197727	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		44285019	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		57514683	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		91898441	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		CHEMBL441738	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		DB04931	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16132144	216058	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		16133793	216058	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		44273719	216058	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		CHEMBL214332	216058	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		1324	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		16154396	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		16197727	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		44285019	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		57514683	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		91898441	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		CHEMBL441738	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		DB04931	7090	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		CHEMBL2369963	216523	0	None	-	0	Mouse	9.6	pEC50	=	9.6	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369967	216527	0	None	-	0	Mouse	9.4	pEC50	=	9.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL365913	218822	0	None	-	0	Human	9.3	pEC50	=	9.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2369975	216535	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369982	216542	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369971	216531	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369960	216520	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369983	216543	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369964	216524	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		118720368	122656	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354737	122656	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720368	122656	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354737	122656	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720369	122657	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354738	122657	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354729	218330	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354736	218334	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		155527254	178029	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
		CHEMBL4460053	178029	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3354729	218330	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354736	218334	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		44322795	213705	0	None	13	3	Human	8.8	pEC50	=	8.8	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL91041	213705	0	None	13	3	Human	8.8	pEC50	=	8.8	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		118720370	122658	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354739	122658	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720370	122658	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354739	122658	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720363	122654	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354732	122654	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720363	122654	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354732	122654	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720364	122655	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354733	122655	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720369	122657	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354738	122657	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720364	122655	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354733	122655	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		16132144	216058	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		16133793	216058	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		44273719	216058	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		CHEMBL214332	216058	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		CHEMBL3354730	218331	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354735	218333	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL188738	215838	0	None	-	0	Human	7.0	pEC50	=	7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL154251	215580	0	None	-	0	Mouse	6.0	pEC50	=	6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm020296e
		CHEMBL330233	218110	0	None	-	0	Mouse	6.0	pEC50	=	6	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354743	218338	0	None	-	0	Human	8.0	pEC50	=	8.0	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		CHEMBL2369961	216521	0	None	-	0	Mouse	6.9	pEC50	=	6.9	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCc3ccccc3C2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL152555	215574	0	None	-	0	Mouse	4.9	pEC50	=	4.9	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm020296e
		CHEMBL275303	217600	0	None	-	0	Mouse	4.9	pEC50	=	4.9	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		101728563	168539	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44308542	168539	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932720	168539	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL413936	168539	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		155551846	181913	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
		CHEMBL4569789	181913	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
		44322868	112785	0	None	-37	3	Human	5.9	pEC50	=	5.9	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313279	112785	0	None	-37	3	Human	5.9	pEC50	=	5.9	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44308622	175654	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932727	175654	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL438237	175654	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		101728568	103537	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		44387459	103537	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		91932729	103537	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL264577	103537	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL190953	215856	0	None	-	0	Human	5.9	pEC50	=	5.9	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL2371827	216911	0	None	-	0	Human	5.9	pEC50	=	5.9	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1021/jm0490033
		CHEMBL317968	217986	0	None	-	0	Mouse	6.9	pEC50	=	6.9	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354724	218329	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354724	218329	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		127047475	146527	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		132991507	146527	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3798421	146527	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL268082	217518	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		127047913	146702	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3799563	146702	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL151906	215573	0	None	-	0	Mouse	6.8	pEC50	=	6.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(N)=O	10.1021/jm020296e
		101728566	168528	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44387460	168528	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932726	168528	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL413842	168528	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL2369968	216528	0	None	-	0	Mouse	4.8	pEC50	=	4.8	Binding	Effective concentration for mouse Melanocortin-4 receptor at 100 uMEffective concentration for mouse Melanocortin-4 receptor at 100 uM	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC1=O	10.1021/jm049010r
		44308621	175692	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932722	175692	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438577	175692	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL357558	218522	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/jm020296e
		CHEMBL348901	218495	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/jm020296e
		CHEMBL3799094	219047	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL320157	218005	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL329490	218096	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL191063	215858	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL191120	215859	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		127047209	146590	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3798845	146590	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
		101728572	168631	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		44387457	168631	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		91932734	168631	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL414723	168631	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL2369972	216532	0	None	-	0	Mouse	4.8	pEC50	=	4.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44369234	52020	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL	685	18	9	7	-0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL152612	52020	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL	685	18	9	7	-0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL264190	217387	1	None	39	2	Mouse	7.8	pEC50	=	7.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354742	218337	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		CHEMBL186970	215833	0	None	-	0	Human	7.7	pEC50	=	7.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		127048118	179786	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL4518266	179786	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL189991	215840	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL190834	215848	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371823	216910	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1021/jm0490033
		CHEMBL2371828	216912	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)C(C)=O	10.1021/jm0490033
		CHEMBL2371832	216914	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL3354730	218331	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354735	218333	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720362	122653	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354731	122653	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720362	122653	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354731	122653	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL373344	218954	0	None	-	0	Human	8.6	pEC50	=	8.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44269217	37033	0	None	-	0	Human	8.5	pEC50	=	8.5	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	649	14	3	6	4.4	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1	10.1021/jm025600i
		CHEMBL13910	37033	0	None	-	0	Human	8.5	pEC50	=	8.5	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	649	14	3	6	4.4	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1	10.1021/jm025600i
		CHEMBL2370154	216580	0	None	1	3	Human	8.5	pEC50	=	8.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm020021z
		10101361	162482	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL405174	162482	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL431092	220401	0	None	-	0	Mouse	6.7	pEC50	=	6.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL329847	218100	0	None	-	0	Mouse	5.7	pEC50	=	5.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		44323212	175498	0	None	-1	2	Human	7.7	pEC50	=	7.7	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		CHEMBL436903	175498	0	None	-1	2	Human	7.7	pEC50	=	7.7	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		44269189	105114	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	587	13	3	6	3.1	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1	10.1021/jm025600i
		CHEMBL275067	105114	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	587	13	3	6	3.1	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1	10.1021/jm025600i
		46877881	208597	0	None	2	3	Human	5.6	pEC50	=	5.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL606990	208597	0	None	2	3	Human	5.6	pEC50	=	5.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		101728569	166510	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44308747	166510	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932733	166510	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL410471	166510	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		101728567	168566	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44387462	168566	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932731	168566	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL414101	168566	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL3354741	218336	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		44308558	175653	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932730	175653	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438228	175653	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		118720357	122651	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354726	122651	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL264190	217387	1	None	39	2	Mouse	6.6	pEC50	=	6.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		118720357	122651	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354726	122651	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL190080	215841	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371835	216916	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL154153	215579	0	None	-	0	Mouse	6.6	pEC50	=	6.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccc2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL2369966	216526	0	None	-	0	Mouse	6.6	pEC50	=	6.6	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44323234	174835	0	None	-7	3	Human	6.6	pEC50	=	6.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL432377	174835	0	None	-7	3	Human	6.6	pEC50	=	6.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		9915813	45263	15	None	-	0	Human	5.6	pEC50	=	5.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	559	12	2	7	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1	10.1021/jm025600i
		CHEMBL14642	45263	15	None	-	0	Human	5.6	pEC50	=	5.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	559	12	2	7	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1	10.1021/jm025600i
		CHEMBL407694	219457	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL347364	218492	0	None	-	0	Mouse	5.6	pEC50	=	5.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/jm020296e
		CHEMBL350012	218501	0	None	-	0	Mouse	4.6	pEC50	=	4.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]cn1)C(N)=O	10.1021/jm020296e
		127047853	146771	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3799955	146771	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL264190	217387	1	None	-	2	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL94369	222687	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL96871	222700	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		118720356	122650	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354725	122650	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720356	122650	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354725	122650	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354722	218327	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		10260053	174982	0	None	-4	3	Human	5.5	pEC50	=	5.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433413	174982	0	None	-4	3	Human	5.5	pEC50	=	5.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433522	220420	0	None	-	0	Mouse	4.5	pEC50	=	4.5	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccncc1)C(N)=O	10.1021/jm020296e
		CHEMBL365262	218816	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL372237	218951	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371833	216915	0	None	-	0	Human	5.5	pEC50	=	5.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2369969	216529	0	None	-	0	Mouse	7.5	pEC50	=	7.5	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44308639	175817	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932721	175817	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL439484	175817	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL2371147	216796	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1	10.1021/jm020296e
		101728564	161944	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		44308543	161944	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		91932719	161944	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL402257	161944	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL2096745	215986	0	None	-	0	Mouse	4.4	pEC50	=	4.4	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/jm020296e
		CHEMBL365794	218820	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190427	215844	0	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL3354722	218327	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		6918707	110969	1	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	110969	1	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL3354734	218332	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354734	218332	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		44269245	174000	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	602	7	2	6	2.8	COc1ccc(C[C@@H](NC(=O)[C@H]2Cc3ccccc3CN2)C(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1	10.1021/jm025600i
		CHEMBL429212	174000	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	602	7	2	6	2.8	COc1ccc(C[C@@H](NC(=O)[C@H]2Cc3ccccc3CN2)C(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1	10.1021/jm025600i
		118720358	122652	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354727	122652	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720358	122652	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354727	122652	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL2369965	216525	0	None	-	0	Mouse	7.4	pEC50	=	7.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369976	216536	0	None	-	0	Mouse	5.4	pEC50	=	5.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2371150	216797	0	None	-	0	Mouse	4.4	pEC50	=	4.4	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(N)=O	10.1021/jm020296e
		71152492	166843	2	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.	ChEMBL	530	12	2	5	3.9	COc1ccc(C[C@@H](NC(=O)CCc2nc[nH]c2C)C(=O)N2CC(OCC3CC3)(c3ccccc3C)C2)cc1	nan
		CHEMBL4108378	166843	2	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.	ChEMBL	530	12	2	5	3.9	COc1ccc(C[C@@H](NC(=O)CCc2nc[nH]c2C)C(=O)N2CC(OCC3CC3)(c3ccccc3C)C2)cc1	nan
		CHEMBL347216	218491	0	None	-	0	Mouse	7.3	pEC50	=	7.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/jm020296e
		16132144	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		16133793	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		44273719	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		CHEMBL214332	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		16132144	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		16133793	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		44273719	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		CHEMBL214332	216058	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		CHEMBL264190	217387	1	None	39	2	Mouse	8.3	pEC50	=	8.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		44322869	112937	0	None	-6	3	Human	7.3	pEC50	=	7.3	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313690	112937	0	None	-6	3	Human	7.3	pEC50	=	7.3	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44360829	172527	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	550	8	3	6	1.3	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL424661	172527	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	550	8	3	6	1.3	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL275999	217605	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL371610	218949	0	None	-	0	Human	5.3	pEC50	=	5.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL94391	222688	0	None	-	0	Mouse	6.3	pEC50	=	6.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL432201	220412	0	None	-	0	Mouse	6.3	pEC50	=	6.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL346925	218490	0	None	-	0	Mouse	5.3	pEC50	=	5.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O	10.1021/jm020296e
		127046235	146416	0	None	-	0	Human	7.3	pEC50	=	7.3	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3797690	146416	0	None	-	0	Human	7.3	pEC50	=	7.3	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
		44308380	103445	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932732	103445	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL263874	103445	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL2304247	216263	0	None	-	0	Mouse	8.2	pEC50	=	8.2	Binding	Displacement of MT2 from mouse MC4R expressed in HEK293 cellsDisplacement of MT2 from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
		CHEMBL3350327	218249	0	None	-	0	Mouse	8.2	pEC50	=	8.2	Binding	Displacement of MT2 from mouse MC4R expressed in HEK293 cellsDisplacement of MT2 from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
		CHEMBL432027	220410	0	None	-	0	Mouse	5.2	pEC50	=	5.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL188459	215836	0	None	-	0	Human	7.2	pEC50	=	7.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		11038873	178659	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	545	12	3	6	2.9	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL446941	178659	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	545	12	3	6	2.9	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL190203	215843	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL370321	218946	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL364711	218811	0	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44387458	175711	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932725	175711	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438749	175711	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		6918707	110969	1	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	110969	1	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		44308379	166993	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932724	166993	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL410966	166993	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		44323233	113493	0	None	4	2	Human	7.2	pEC50	=	7.2	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL314401	113493	0	None	4	2	Human	7.2	pEC50	=	7.2	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL327479	218073	0	None	-	0	Mouse	7.2	pEC50	=	7.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL2369970	216530	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		11828678	214652	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	721	16	8	6	1.0	CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm0104872
		CHEMBL96531	214652	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	721	16	8	6	1.0	CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm0104872
		CHEMBL2369962	216522	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44269214	105270	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	546	12	3	6	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL276012	105270	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	546	12	3	6	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL152986	215576	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccccc1)C(N)=O	10.1021/jm020296e
		CHEMBL358833	218582	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm020296e
		CHEMBL190551	215845	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190732	215846	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2371829	216913	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL3354723	218328	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354723	218328	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL349795	218499	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccs1)C(N)=O	10.1021/jm020296e
		CHEMBL3354740	218335	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		11813437	105305	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	530	12	2	5	4.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL276301	105305	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	530	12	2	5	4.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL2096693	215983	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/jm020296e
		CHEMBL2369977	216537	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2371147	216796	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1	10.1021/jm020296e
		CHEMBL317969	217987	0	None	-	0	Mouse	6.1	pEC50	=	6.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		44308666	175641	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932723	175641	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL438160	175641	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL330561	218112	0	None	-	0	Mouse	7.0	pEC50	=	7.0	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cccs1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL2096742	215985	0	None	5	2	Human	10.2	pIC50	=	10.2	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0202526
		CHEMBL1161322	215287	0	None	1	2	Human	10.1	pIC50	=	10.1	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		6918780	70241	1	None	-	0	Human	10.0	pIC50	=	10	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL179836	70241	1	None	-	0	Human	10.0	pIC50	=	10	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		1324	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		16154396	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		16197727	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		44285019	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		57514683	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		91898441	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		CHEMBL441738	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		DB04931	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		1324	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		16154396	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		16197727	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		44285019	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		57514683	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		91898441	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		CHEMBL441738	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		DB04931	7090	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		CHEMBL1161323	215288	0	None	5	2	Human	9.8	pIC50	=	9.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O	10.1021/jm0202526
		122194229	130761	0	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3629347	130761	0	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		1324	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		16154396	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		16197727	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		44285019	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		57514683	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		91898441	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		CHEMBL441738	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		DB04931	7090	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		72548703	168346	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		CHEMBL4128926	168346	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		44366081	17034	0	None	2	2	Human	9.6	pIC50	=	9.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL1161313	17034	0	None	2	2	Human	9.6	pIC50	=	9.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL2369484	216406	0	None	-	0	Mouse	9.6	pIC50	=	9.6	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		11061068	38066	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL140154	38066	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		11061068	38066	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
		CHEMBL140154	38066	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
		10304547	175031	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL433764	175031	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		1324	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16154396	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16197727	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		44285019	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		57514683	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		91898441	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL441738	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		DB04931	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		1324	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		16154396	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		16197727	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		44285019	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		57514683	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		91898441	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		CHEMBL441738	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		DB04931	7090	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		50899078	24926	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269573	24926	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		16746823	24929	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269576	24929	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1161318	215284	0	None	79	2	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O	10.1021/jm0202526
		1324	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16154396	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16197727	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44285019	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		57514683	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		91898441	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		CHEMBL441738	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		DB04931	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44366171	128072	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm0202526
		CHEMBL358015	128072	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm0202526
		16725559	101764	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254757	101764	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		122184910	129333	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601428	129333	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		10864861	121978	4	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL334457	121978	4	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL1161316	215283	0	None	63	2	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O	10.1021/jm0202526
		1324	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16154396	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16197727	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44285019	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		57514683	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		91898441	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		CHEMBL441738	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		DB04931	7090	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		56659456	70475	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801215	70475	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
		44397455	130621	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL362523	130621	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL2096742	215985	0	None	5	2	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm801300c
		CHEMBL500743	220903	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		1338	10579	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	10579	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	10579	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		44408154	148140	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
		CHEMBL383719	148140	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
		44417552	148356	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL384955	148356	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		56673302	70445	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801095	70445	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		1323	9465	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		92432	9465	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		CHEMBL430239	9465	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		6918849	129742	1	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL360818	129742	1	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		54587278	67592	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	587	6	3	4	4.7	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1762009	67592	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	587	6	3	4	4.7	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		44408286	147446	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL381501	147446	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		16746686	24928	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269575	24928	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		44441641	101076	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL250508	101076	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		56676638	70467	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801146	70467	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
		56666386	70476	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801216	70476	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL2115441	216047	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		49862736	21909	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209787	21909	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44408173	82176	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL203975	82176	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL2369484	216406	0	None	-	0	Mouse	9.0	pIC50	=	9.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		24857886	162027	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402769	162027	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		49862748	21921	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209799	21921	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL393075	219241	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2007.02.020
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		1324	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		16154396	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		16197727	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		44285019	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		57514683	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		91898441	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		CHEMBL441738	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		DB04931	7090	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		10304776	85754	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	6.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL2113041	85754	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	6.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		10282847	129743	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	5.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL360819	129743	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	5.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1	10.1016/j.bmcl.2005.05.012
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		56669819	70465	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801144	70465	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		1323	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		92432	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		CHEMBL430239	9465	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		1324	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		16154396	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		16197727	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		44285019	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		57514683	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		91898441	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		CHEMBL441738	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		DB04931	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		1324	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		16154396	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		16197727	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		44285019	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		57514683	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		91898441	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		CHEMBL441738	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		DB04931	7090	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		1338	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		9938402	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		CHEMBL339053	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		44358565	36799	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
		CHEMBL138901	36799	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
		1338	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		9938402	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		CHEMBL339053	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		44418431	143334	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
		CHEMBL373821	143334	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
		CHEMBL503229	220942	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
		1338	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		1338	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		11017471	38691	0	None	-	1	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
		CHEMBL140738	38691	0	None	-	1	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
		1338	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	10579	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL443071	220699	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		CHEMBL1161321	215286	0	None	19	2	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1021/jm0202526
		1324	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16154396	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16197727	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44285019	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		57514683	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		91898441	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		CHEMBL441738	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		DB04931	7090	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44408287	82161	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL203911	82161	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		52943061	24920	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269568	24920	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		56683301	70471	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801150	70471	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
		56662904	70477	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801217	70477	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		49862750	21924	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209801	21924	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
		44349223	120577	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	673	11	0	7	3.7	CCOC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL332443	120577	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	673	11	0	7	3.7	CCOC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3348530	218181	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1016/j.bmcl.2003.10.056
		44310344	104104	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231883	104104	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL269274	104104	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44347840	168703	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		91932630	168703	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		CHEMBL415333	168703	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		44448631	101845	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL255286	101845	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL501592	220920	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		15953833	85749	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	85749	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		15953833	85749	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	85749	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		56669820	70468	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
		CHEMBL1801147	70468	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
		56676639	70470	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801149	70470	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
		49862749	21923	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209800	21923	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
		44448629	174242	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL429854	174242	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		52941830	24927	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269574	24927	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		56659468	70466	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801145	70466	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		56679968	70469	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801148	70469	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
		1323	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		92432	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		CHEMBL430239	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		CHEMBL385976	219150	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL2096742	215985	0	None	5	2	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm070461w
		CHEMBL266417	217462	0	None	8	3	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
		10210964	74017	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	606	7	3	4	5.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL187990	74017	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	606	7	3	4	5.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		132938008	166292	0	None	17	3	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4102048	166292	0	None	17	3	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		52945472	24921	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269569	24921	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		44357786	123532	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL337571	123532	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10119206	125554	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL341982	125554	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		1324	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16154396	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16197727	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44285019	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		57514683	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		91898441	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		CHEMBL441738	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		DB04931	7090	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		145994283	174157	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	680	14	5	5	2.9	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4294862	174157	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	680	14	5	5	2.9	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL2373991	217160	0	None	5	2	Mouse	8.0	pIC50	=	8	Binding	Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/jm049620r
		127047336	146576	0	None	-1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798768	146576	0	None	-1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423463	92171	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226281	92171	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		127047624	146674	0	None	1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799408	146674	0	None	1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		145972289	171299	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4214826	171299	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		122184635	129212	0	None	-1	4	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600916	129212	0	None	-1	4	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44457043	104388	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL270923	104388	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44423467	92196	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	584	10	0	4	7.1	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(C)(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226391	92196	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	584	10	0	4	7.1	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(C)(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44383343	127120	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21	10.1021/jm0309452
		CHEMBL353007	127120	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21	10.1021/jm0309452
		44397653	73766	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186876	73766	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397445	130410	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(C(F)(F)F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361881	130410	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(C(F)(F)F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL425591	220117	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
		71456236	85665	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2112918	85665	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		155546131	180309	0	None	-2	3	Mouse	6.0	pIC50	=	6	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4531291	180309	0	None	-2	3	Mouse	6.0	pIC50	=	6	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL190732	215846	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2371963	216939	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0614275
		44397337	74156	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188720	74156	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL203760	215940	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0510326
		44373317	126436	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL346930	126436	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		155551202	180738	0	None	-	0	Mouse	5.0	pIC50	=	5	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4541505	180738	0	None	-	0	Mouse	5.0	pIC50	=	5	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44417554	175618	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	867	15	10	9	-0.7	CC(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL437899	175618	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	867	15	10	9	-0.7	CC(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		44448477	102332	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257615	102332	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		122184576	129206	0	None	-	1	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600837	129206	0	None	-	1	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		155561116	181752	0	None	1	4	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4566163	181752	0	None	1	4	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44310259	168479	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932914	168479	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL413465	168479	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		10123761	106269	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determinedBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determined	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL283214	106269	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determinedBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determined	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		44423430	92009	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225693	92009	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600921	218603	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44361027	38068	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm049278i
		CHEMBL140155	38068	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm049278i
		44361027	38068	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL140155	38068	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		10232394	125956	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	599	13	2	7	3.3	CN(C)CCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343076	125956	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	599	13	2	7	3.3	CN(C)CCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10483153	67585	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761873	67585	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL501642	220921	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		44397410	131137	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363740	131137	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349224	23320	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	10	0	6	3.1	CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL123744	23320	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	10	0	6	3.1	CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		10145026	19041	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184727	19041	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028962	19041	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		44448590	102374	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257759	102374	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		10239507	92055	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226025	92055	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423457	92142	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226176	92142	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		49862739	21913	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209791	21913	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		44357528	125054	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	680	14	1	6	6.9	O=C(CCN(Cc1ccccc1)Cc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL340959	125054	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	680	14	1	6	6.9	O=C(CCN(Cc1ccccc1)Cc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		71461649	85729	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113007	85729	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL410795	219621	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		CHEMBL397413	219283	6	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.04.001
		44397535	179554	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL451249	179554	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44348200	166975	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		CHEMBL410949	166975	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		122184575	129205	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600836	129205	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44441647	161469	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL399714	161469	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL264190	217387	1	None	-	2	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		9917301	92200	2	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226443	92200	2	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10973172	176060	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL441342	176060	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		44423428	92007	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225691	92007	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44358915	19849	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1190181	19849	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL540320	19849	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		10146090	34818	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	639	13	2	7	4.2	O=C(CCN1CCCCC1)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137273	34818	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	639	13	2	7	4.2	O=C(CCN1CCCCC1)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10165866	125783	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	542	10	2	6	3.4	CC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL342590	125783	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	542	10	2	6	3.4	CC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44357167	175297	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL435400	175297	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL2386882	217173	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to MC4R in HEK293 cellsBinding affinity to MC4R in HEK293 cells	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1016/j.bmcl.2013.02.022
		56673304	70454	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801120	70454	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
		56669817	70456	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801122	70456	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
		54584302	67586	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761874	67586	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
		10098971	130802	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	130802	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		56658412	72686	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930590	72686	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835942	72686	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		71454491	85728	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113006	85728	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		44373197	126251	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL345234	126251	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44422999	175634	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL	1040	15	9	10	3.0	CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL438118	175634	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL	1040	15	9	10	3.0	CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL264190	217387	1	None	39	2	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		4189	213701	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	213701	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	213701	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		44358566	171662	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL422109	171662	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423426	150385	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389957	150385	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL1172251	215362	0	None	-	4	Human	5.9	pIC50	=	5.9	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		168278924	197845	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5187368	197845	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		10952071	38004	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL140108	38004	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		44448436	102377	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257770	102377	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		9919056	147847	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
		CHEMBL382511	147847	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
		10210972	19047	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL1184771	19047	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145454	19047	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		132180598	164628	0	None	-	1	Mouse	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4083717	164628	0	None	-	1	Mouse	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		11753695	15165	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1093304	15165	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		10077258	21803	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209253	21803	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		11753695	15165	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093304	15165	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397412	74085	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188395	74085	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349469	23865	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125492	23865	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44448661	101774	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254792	101774	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44441681	100904	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249319	100904	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		44358660	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL435697	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL544851	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		49862376	21812	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209319	21812	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		44397702	130863	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363280	130863	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358660	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL435697	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL544851	175338	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349026	123778	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	2	6	2.9	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCNCC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338811	123778	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	2	6	2.9	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCNCC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3754655	219002	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL1172251	215362	0	None	-	4	Human	5.9	pIC50	=	5.9	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		71459937	85750	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113038	85750	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2371928	216933	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2006.07.036
		22318631	92027	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	532	10	1	5	5.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(O)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225965	92027	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	532	10	1	5	5.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(O)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423437	143614	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	504	9	0	4	5.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Cl)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL374176	143614	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	504	9	0	4	5.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Cl)cc2)CC1	10.1016/j.bmc.2006.12.039
		155561116	181752	0	None	-1	4	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4566163	181752	0	None	-1	4	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		122184578	129208	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600839	129208	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		137651071	164246	0	None	-	1	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4079298	164246	0	None	-	1	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		176	7186	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	7186	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	7186	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	7186	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	7186	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		122184577	129207	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600838	129207	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600834	218594	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44357527	125672	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	590	12	2	6	5.0	O=C(CCNCc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL342268	125672	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	590	12	2	6	5.0	O=C(CCNCc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44447251	161577	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
		CHEMBL400237	161577	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
		56661897	72690	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930594	72690	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835946	72690	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL2331674	216311	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml300312b
		1324	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16154396	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16197727	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44285019	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		57514683	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		91898441	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		CHEMBL441738	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		DB04931	7090	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44396987	73967	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL187774	73967	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		44423384	19629	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188648	19629	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL536977	19629	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		2247	7293	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	7293	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	7293	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	7293	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	7293	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		155532232	178484	0	None	2	3	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4466724	178484	0	None	2	3	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358698	37697	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139803	37697	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423432	92011	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	10	0	4	5.4	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225749	92011	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	10	0	4	5.4	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44441634	100786	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	478	6	2	4	3.6	CC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248700	100786	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	478	6	2	4	3.6	CC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		131839615	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		44275263	168705	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL415341	168705	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		10077258	21803	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209253	21803	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		49862664	21895	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209706	21895	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44423460	92155	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226228	92155	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL186970	215833	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		44277696	107982	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
		CHEMBL29582	107982	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
		10373417	107582	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		CHEMBL29317	107582	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		44277696	107982	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
		CHEMBL29582	107982	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
		49862426	21833	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209383	21833	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
		10973172	176060	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL441342	176060	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL203170	215937	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC1=O	10.1021/jm0510326
		44372933	126691	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL349298	126691	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		49862744	21917	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209795	21917	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		11730771	22028	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		CHEMBL12120	22028	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		10481801	23629	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12487	23629	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		2726	7706	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	7706	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	7706	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	7706	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	7706	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		44423452	92086	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(-c4ccccc4)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226073	92086	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(-c4ccccc4)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		155551202	180738	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4541505	180738	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL1172249	215361	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172253	215364	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL190080	215841	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190953	215856	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL2371835	216916	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		49798107	17618	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933502	17618	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172247	17618	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		44423440	92018	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Br)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225854	92018	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Br)cc2)CC1	10.1016/j.bmc.2006.12.039
		10128451	122925	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	512	8	2	6	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)C1CNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL335779	122925	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	512	8	2	6	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)C1CNC1	10.1016/j.bmcl.2003.09.036
		10141778	123497	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL337351	123497	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		131839615	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	219415	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		6918813	138149	3	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	138149	3	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		54584301	67584	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
		CHEMBL1761872	67584	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
		71452720	85746	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL2113031	85746	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		52944242	24925	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269572	24925	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
		CHEMBL204864	215945	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
		CHEMBL3600832	218592	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44441639	100825	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248893	100825	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		9842665	163585	12	None	-3	2	Human	6.8	pIC50	=	6.8	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
		CHEMBL40711	163585	12	None	-3	2	Human	6.8	pIC50	=	6.8	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
		CHEMBL1172249	215361	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172253	215364	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		145977650	170613	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4206406	170613	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2371966	216942	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0614275
		24774358	161683	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	811	9	10	8	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL400866	161683	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	811	9	10	8	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44397460	132997	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365004	132997	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44396125	73058	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	374	5	1	2	4.8	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL184736	73058	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	374	5	1	2	4.8	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL2371973	216949	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/jm0614275
		CHEMBL375947	219011	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44441685	100907	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249322	100907	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		10481801	23629	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12487	23629	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44397700	74098	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc4ccccc4c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188451	74098	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc4ccccc4c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2096759	215987	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401323	18572	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1181891	18572	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028961	18572	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44448698	101707	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254351	101707	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL409144	219526	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm0510326
		CHEMBL446185	220723	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
		CHEMBL3600913	218601	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44431513	152587	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1054	14	12	10	1.4	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		CHEMBL391704	152587	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1054	14	12	10	1.4	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		44348183	103940	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1493	31	14	21	-0.8	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL268094	103940	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1493	31	14	21	-0.8	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		44441638	161159	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	504	7	2	4	4.0	N#CCC1(C2CC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398717	161159	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	504	7	2	4	4.0	N#CCC1(C2CC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44441683	100905	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249320	100905	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		44423431	92010	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CCCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225748	92010	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CCCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10951027	23614	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL12480	23614	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		122184912	129336	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601430	129336	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44357294	34975	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	4.0	CC(C)(N)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137367	34975	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	4.0	CC(C)(N)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		71449119	85743	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL2113028	85743	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
		49862375	21811	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209318	21811	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		49862377	21813	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209320	21813	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		168273822	197349	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5180152	197349	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44423449	92054	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	10	0	5	6.1	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226024	92054	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	10	0	5	6.1	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		71456245	85751	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113039	85751	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		122184499	129171	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1088	17	13	11	0.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600737	129171	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1088	17	13	11	0.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44423378	19613	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188561	19613	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL536747	19613	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44357547	34895	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	596	10	2	6	3.9	O=C(CCNC(=O)C(F)(F)F)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137318	34895	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	596	10	2	6	3.9	O=C(CCNC(=O)C(F)(F)F)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL413573	219854	0	None	-	2	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
		44396126	72887	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	404	5	1	2	5.6	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nc(C)c[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL183954	72887	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	404	5	1	2	5.6	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nc(C)c[nH]1	10.1016/j.bmcl.2004.08.055
		44423450	92053	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	9	0	4	5.4	CC(C)N1CCN(C(CN2CCN(CCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226023	92053	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	9	0	4	5.4	CC(C)N1CCN(C(CN2CCN(CCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423427	92206	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226502	92206	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		122184909	129332	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601427	129332	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		11092574	25582	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		CHEMBL12783	25582	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		131839615	219415	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	219415	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	219415	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16132144	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		16133793	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		44273719	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		CHEMBL214332	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		16132144	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		16133793	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		44273719	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		CHEMBL214332	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		44397660	130209	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361731	130209	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349228	25587	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL127861	25587	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		16132144	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		16133793	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		44273719	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		CHEMBL214332	216058	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		24764421	19952	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1190957	19952	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL541897	19952	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		16721030	19675	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188987	19675	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL537873	19675	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL373344	218954	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44358630	35087	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137452	35087	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL541866	35087	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL3752534	218995	1	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL417853	220017	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		155536962	179016	0	None	1	2	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4474215	179016	0	None	1	2	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		10008561	21788	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209192	21788	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL417853	220017	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory activity against hMC4R (human melanocortin receptor) using I-AGRP as radioligandInhibitory activity against hMC4R (human melanocortin receptor) using I-AGRP as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		10928744	23564	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12457	23564	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		155536962	179016	0	None	-1	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4474215	179016	0	None	-1	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358609	35552	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137855	35552	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1172619	215367	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL408509	219499	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		CHEMBL364711	218811	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		1323	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		92432	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		CHEMBL430239	9465	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		1324	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		16154396	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		16197727	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		44285019	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		57514683	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		91898441	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		CHEMBL441738	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		DB04931	7090	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		56679956	70474	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801214	70474	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		46919520	21910	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209788	21910	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44349471	23645	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL124954	23645	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL410217	219587	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		56683299	70463	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801142	70463	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		145980838	173445	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	670	14	5	5	3.1	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4281687	173445	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	670	14	5	5	3.1	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		44408155	147331	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
		CHEMBL381125	147331	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
		56676632	70452	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801118	70452	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		44358639	36764	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	526	8	2	7	3.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NC3CCCCNC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL138878	36764	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	526	8	2	7	3.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NC3CCCCNC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		56676614	70478	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801218	70478	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		1323	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		92432	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		CHEMBL430239	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		1323	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		92432	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		CHEMBL430239	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		1323	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		92432	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		CHEMBL430239	9465	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		49862747	21920	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209798	21920	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL3600736	218591	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		49862745	21918	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
		CHEMBL1209796	21918	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
		49862751	21925	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209802	21925	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
		44397569	129684	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360602	129684	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		56676631	70443	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801093	70443	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		56676635	70461	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801127	70461	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL502300	220931	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		CHEMBL428801	220251	0	None	-3	3	Human	8.6	pIC50	=	8.6	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
		CHEMBL365913	218822	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		56659466	70447	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801097	70447	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		56673305	70457	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
		CHEMBL1801123	70457	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
		56659467	70460	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
		CHEMBL1801126	70460	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
		56683300	70464	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801143	70464	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		49862665	21896	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209707	21896	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44391929	19184	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1185810	19184	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145453	19184	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL414778	219935	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401315	19053	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184825	19053	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028957	19053	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		10123761	106269	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL283214	106269	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL1172619	215367	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		118735101	125579	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421678	125579	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		118735103	125581	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421680	125581	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		11757528	21789	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209193	21789	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		44397654	73962	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL187761	73962	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		155532232	178484	0	None	-2	3	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4466724	178484	0	None	-2	3	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44431512	152702	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		CHEMBL391796	152702	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		127053937	155832	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	502	11	2	4	4.3	CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O	nan
		CHEMBL3942822	155832	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	502	11	2	4	4.3	CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O	nan
		122184633	129210	0	None	-	1	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600914	129210	0	None	-	1	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44358693	19831	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1190075	19831	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL540077	19831	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423422	92199	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226442	92199	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL432895	220414	4	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		44357406	126053	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	572	12	2	7	3.0	COCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343742	126053	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	572	12	2	7	3.0	COCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		127046262	146598	0	None	1	3	Mouse	7.7	pIC50	=	7.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798912	146598	0	None	1	3	Mouse	7.7	pIC50	=	7.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44390411	70670	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL180487	70670	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL417853	220017	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		CHEMBL264190	217387	1	None	39	2	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		10874535	23293	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		CHEMBL12369	23293	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		16725558	162448	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL404905	162448	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		10004020	25620	2	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12811	25620	2	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44358669	20599	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1195769	20599	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL555316	20599	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423424	92202	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CN1CCN(C(CN2CCN(CCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226496	92202	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CN1CCN(C(CN2CCN(CCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44357280	34434	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL136993	34434	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44357626	126052	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	9	2	6	4.0	O=C(C[C@@H]1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343720	126052	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	9	2	6	4.0	O=C(C[C@@H]1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		22318636	92028	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	12	0	5	6.5	CC(C)Oc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225966	92028	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	12	0	5	6.5	CC(C)Oc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		10098971	130802	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	130802	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		71459938	85756	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	85756	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		71459938	85756	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	85756	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44373198	58940	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL158808	58940	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44441636	100787	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248701	100787	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44448554	162151	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403421	162151	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		56668797	72685	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930589	72685	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835941	72685	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		132180599	163672	0	None	-	1	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4072129	163672	0	None	-	1	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
		118735102	125580	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421679	125580	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		44349226	123761	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338747	123761	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3349030	218184	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		155566718	182695	0	None	3	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4587214	182695	0	None	3	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358697	19734	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1189383	19734	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL538589	19734	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423442	92021	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	538	9	0	4	5.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225909	92021	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	538	9	0	4	5.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423468	90248	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	604	11	0	4	7.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL220092	90248	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	604	11	0	4	7.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423445	92026	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc(CCCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)c2ccccc12	10.1016/j.bmc.2006.12.039
		CHEMBL225964	92026	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc(CCCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)c2ccccc12	10.1016/j.bmc.2006.12.039
		49862378	21814	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209321	21814	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		44423454	92102	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226123	92102	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL508501	221721	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		44423382	20720	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196602	20720	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL557585	20720	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44423462	92170	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226280	92170	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2372623	217056	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		44423438	92015	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2Br)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225800	92015	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2Br)CC1	10.1016/j.bmc.2006.12.039
		11050211	41596	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL143131	41596	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		11050211	41596	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL143131	41596	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		44401321	18568	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1181867	18568	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028960	18568	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44423459	92154	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226227	92154	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		44423433	92201	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	556	10	0	4	6.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CCCCC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL226444	92201	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	556	10	0	4	6.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CCCCC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44423453	92087	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226074	92087	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600842	218598	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		11092487	169367	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL416890	169367	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44357348	126117	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL344231	126117	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10373417	107582	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		CHEMBL29317	107582	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		6918780	70241	1	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL179836	70241	1	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		90661465	83937	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		CHEMBL2028958	83937	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		CHEMBL2078649	83937	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		155548853	180588	0	None	3	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4538274	180588	0	None	3	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL427205	220131	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
		CHEMBL1172252	215363	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL2372623	217056	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL188738	215838	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL191120	215859	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL3799094	219047	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL103817	215238	0	None	1	3	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423446	144930	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	12	0	5	6.1	CCOc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL376829	144930	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	12	0	5	6.1	CCOc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		15953833	85749	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	85749	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL1172252	215363	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		133053557	170485	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4204975	170485	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		10098568	21790	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209194	21790	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		22318671	92022	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	515	10	0	6	4.7	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225910	92022	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	515	10	0	6	4.7	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmc.2006.12.039
		10951027	23614	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL12480	23614	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		49862425	21832	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209382	21832	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		44423456	92106	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226125	92106	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423458	92143	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3c(Cl)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226177	92143	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3c(Cl)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL1161320	215285	0	None	-12	2	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O	10.1021/jm0202526
		CHEMBL526334	222460	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
		CHEMBL263822	217369	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
		155546131	180309	0	None	2	3	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4531291	180309	0	None	2	3	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL381739	219071	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0510326
		137653916	165359	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4091894	165359	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL2096710	215984	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049620r
		44358608	37068	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139126	37068	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		10257242	21802	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209252	21802	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		10188529	133559	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL365401	133559	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		44397659	73893	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL187450	73893	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397534	74042	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188142	74042	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397338	130455	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL362129	130455	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44448515	162223	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403834	162223	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		44390422	70242	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL179837	70242	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		71459937	85750	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113038	85750	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		11092487	169367	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL416890	169367	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		10257242	21802	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209252	21802	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		44390424	70701	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180635	70701	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		44401319	19054	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184826	19054	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028959	19054	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44310103	173426	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231882	173426	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL428134	173426	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44397339	74248	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@@H]3CNCC[C@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL189236	74248	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@@H]3CNCC[C@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2369485	216407	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		127047913	146702	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799563	146702	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423441	92019	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	484	9	0	4	5.1	Cc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225855	92019	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	484	9	0	4	5.1	Cc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		44358917	19810	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1189954	19810	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL539813	19810	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL217305	216152	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1016/s0960-894x(03)00412-8
		44349221	103272	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	655	12	0	6	4.0	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(CC3CC3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL262512	103272	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	655	12	0	6	4.0	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(CC3CC3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		11273288	19732	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL1189370	19732	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL538567	19732	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		44401520	20702	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1196472	20702	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL557154	20702	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		56662925	70450	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801116	70450	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		101880965	168733	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		44426646	168733	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971099	168733	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL415660	168733	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		44397409	129722	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360717	129722	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1324	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16154396	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16197727	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		44285019	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		57514683	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		91898441	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		CHEMBL441738	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		DB04931	7090	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		44426648	174367	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971095	174367	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL430079	174367	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		16725559	101764	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254757	101764	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		44349222	120576	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	701	10	0	7	4.5	CC(C)(C)OC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL332442	120576	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	701	10	0	7	4.5	CC(C)(C)OC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		71449047	85255	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2111807	85255	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2372588	217051	0	None	316	2	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O	10.1021/jm0202526
		44441643	161579	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL400252	161579	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		49862746	21919	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209797	21919	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		1324	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		16154396	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		16197727	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		44285019	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		57514683	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		91898441	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		CHEMBL441738	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		DB04931	7090	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		CHEMBL2372589	217052	0	None	-15	2	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0202526
		44441644	161617	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL400456	161617	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44397444	130413	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361890	130413	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44426647	149787	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971098	149787	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL389469	149787	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		56662927	70462	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
		CHEMBL1801141	70462	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
		122184637	129214	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600918	129214	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		10230144	37168	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	3.8	CC(C)(CN)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL139217	37168	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	3.8	CC(C)(CN)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44391940	19022	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1184624	19022	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145456	19022	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		73345549	96226	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371218	96226	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44445085	103849	0	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	879	9	11	9	1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL267265	103849	0	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	879	9	11	9	1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		11215758	72853	0	None	125	3	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration against Melanocortin 4 receptorInhibitory concentration against Melanocortin 4 receptor	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183799	72853	0	None	125	3	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration against Melanocortin 4 receptorInhibitory concentration against Melanocortin 4 receptor	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		44372964	58521	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL158471	58521	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		1337	10197	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	10197	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	10197	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		1337	10197	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	10197	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	10197	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		22318657	92008	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	9	1	4	4.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCNCC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225692	92008	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	9	1	4	4.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCNCC2)cc1	10.1016/j.bmc.2006.12.039
		122184911	129334	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601429	129334	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		1016	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	10519	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		10886436	125935	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL342954	125935	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		49862662	21893	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209704	21893	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1172246	215360	0	None	-	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O	10.1016/j.bmcl.2010.05.078
		56682297	72692	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930595	72692	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835948	72692	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		10098133	21787	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209191	21787	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL417853	220017	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		CHEMBL417853	220017	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibitory activity against hMC4R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligandInhibitory activity against hMC4R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		44310242	163088	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932912	163088	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL406550	163088	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		122184914	129337	0	None	-	1	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601432	129337	0	None	-	1	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL191063	215858	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL372237	218951	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL189991	215840	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		44441648	161470	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL399715	161470	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL1172246	215360	0	None	-	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O	10.1016/j.bmcl.2010.05.078
		44349470	23705	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125308	23705	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		155544852	181718	0	None	1	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4565367	181718	0	None	1	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL3600841	218597	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		145966716	171084	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212209	171084	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2370695	216691	0	None	2	2	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		10928744	23564	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12457	23564	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		11016325	23298	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	480	6	0	5	3.7	CN1CCN(C(CN2CCN(CC3CCc4ccccc4C3=O)CC2)c2ccc(Cl)cc2)CC1	10.1021/jm0255522
		CHEMBL12370	23298	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	480	6	0	5	3.7	CN1CCN(C(CN2CCN(CC3CCc4ccccc4C3=O)CC2)c2ccc(Cl)cc2)CC1	10.1021/jm0255522
		57854192	159828	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	576	11	5	4	4.2	N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O	nan
		CHEMBL3975851	159828	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	576	11	5	4	4.2	N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O	nan
		15953838	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL188146	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL539306	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL4299619	220374	0	None	-	0	Mouse	7.5	pIC50	=	7.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423455	92103	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226124	92103	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL194552	215878	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		15953838	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188146	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL539306	74044	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44445083	161084	0	None	-	1	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	953	9	10	9	2.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL398665	161084	0	None	-	1	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	953	9	10	9	2.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		91971097	122046	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1381	51	15	16	6.7	CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL3348561	122046	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1381	51	15	16	6.7	CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmcl.2007.04.001
		44347927	164055	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1443	31	14	21	-1.9	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL407680	164055	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1443	31	14	21	-1.9	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL1201469	21279	0	None	-2	4	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		None	nan
		44423359	20666	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196208	20666	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL556164	20666	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44423429	143993	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL375057	143993	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		11733360	105152	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL275299	105152	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44358705	103400	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL263461	103400	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL383250	219091	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0510326
		49798104	17617	0	None	-	3	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172244	17617	0	None	-	3	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		9808720	70996	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180892	70996	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		44423425	150384	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CN1CCN(C(CN2CCN(CCCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389956	150384	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CN1CCN(C(CN2CCN(CCCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44441689	161197	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL398932	161197	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		127053935	150963	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	602	11	2	4	6.2	O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1	nan
		CHEMBL3904191	150963	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	602	11	2	4	6.2	O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1	nan
		49862376	21812	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209319	21812	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		10122170	137097	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	638	10	3	7	2.2	CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL368008	137097	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	638	10	3	7	2.2	CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2310901	216277	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		73350149	96228	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371220	96228	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		6918707	110969	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	110969	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL264190	217387	1	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		22318643	92023	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	485	9	1	5	4.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(N)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225911	92023	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	485	9	1	5	4.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(N)cc2)CC1	10.1016/j.bmc.2006.12.039
		44397651	73725	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186675	73725	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44441687	100780	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL248671	100780	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		44423461	92169	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226279	92169	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423444	144898	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	594	10	0	4	6.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(Br)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL376609	144898	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	594	10	0	4	6.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(Br)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL227239	216230	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		11092574	25582	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		CHEMBL12783	25582	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		44448628	161896	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402009	161896	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		145976444	170742	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4207858	170742	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		71456219	85522	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2112603	85522	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		71456220	85523	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1483	33	16	22	-2.5	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2112604	85523	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1483	33	16	22	-2.5	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		155548853	180588	0	None	-3	4	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4538274	180588	0	None	-3	4	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL263948	217378	1	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960840h
		16132144	216058	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		16133793	216058	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		44273719	216058	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		CHEMBL214332	216058	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		44358630	35087	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137452	35087	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL541866	35087	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		11811937	24742	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	424	8	0	4	3.4	CN1CCN(C(CN2CCN(CCCc3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12615	24742	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	424	8	0	4	3.4	CN1CCN(C(CN2CCN(CCCc3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL444493	220712	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		46884748	15168	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093307	15168	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397459	132572	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364789	132572	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358633	20615	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1195894	20615	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL555546	20615	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		49798104	17617	0	None	-	3	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172244	17617	0	None	-	3	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		49798108	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933501	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172248	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL370321	218946	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL371610	218949	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		44441645	100902	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL249277	100902	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44408190	103698	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL265985	103698	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44448629	174242	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL429854	174242	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL2371712	216888	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		73354641	96227	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371219	96227	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44401522	19556	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188041	19556	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL534928	19556	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		44448631	101845	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL255286	101845	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44417551	148221	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL384166	148221	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		1324	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		16154396	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		16197727	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		44285019	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		57514683	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		91898441	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		CHEMBL441738	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		DB04931	7090	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		11215553	15166	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093305	15166	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44408189	175658	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
		CHEMBL438259	175658	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
		44349593	125167	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL341055	125167	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44310344	104104	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231883	104104	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL269274	104104	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		11215553	15166	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1093305	15166	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44408275	82194	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL204078	82194	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		44408276	82282	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL204308	82282	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		9808801	67583	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761871	67583	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		44397356	73691	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186557	73691	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397698	132979	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364992	132979	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44310103	173426	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231882	173426	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL428134	173426	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44408252	147447	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL381503	147447	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44349247	123767	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	671	13	0	6	4.6	CC(C)CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338767	123767	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	671	13	0	6	4.6	CC(C)CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		52918026	67582	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761870	67582	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL2386883	217174	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to MC4R in HEK293 cellsBinding affinity to MC4R in HEK293 cells	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2013.02.022
		44401313	19059	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184856	19059	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028956	19059	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		22318635	20762	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196957	20762	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL558789	20762	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		579	9918	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		6918468	9918	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		CHEMBL41547	9918	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		44426652	173235	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		91971096	173235	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		CHEMBL427795	173235	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		49798107	17618	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933502	17618	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172247	17618	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		44348144	164601	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL408336	164601	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		10348630	36969	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139042	36969	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44396986	74206	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL188966	74206	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		44423465	92182	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL226342	92182	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44275312	148185	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL384036	148185	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		56661653	72387	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930588	72387	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1833974	72387	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		44390421	70680	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180544	70680	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
		44310243	175966	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932909	175966	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL440633	175966	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		44423466	173111	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL427270	173111	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		10213106	79201	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
		CHEMBL198772	79201	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
		137649368	164185	0	None	-	1	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4078495	164185	0	None	-	1	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		44397570	129687	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360603	129687	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3349030	218184	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		24774519	101629	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	911	9	10	8	2.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL253788	101629	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	911	9	10	8	2.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		71456246	85753	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113040	85753	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		145964837	171126	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212629	171126	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		49862740	21914	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209792	21914	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		49798108	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933501	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172248	17619	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		118735099	125577	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421676	125577	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		44397655	74081	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188360	74081	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397658	132204	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364582	132204	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1334	8283	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16133814	8283	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL437050	8283	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL411359	219658	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		168274393	196884	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5172938	196884	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL376339	219023	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		137658359	166350	0	None	-	1	Mouse	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4102774	166350	0	None	-	1	Mouse	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL2331673	216310	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)CCNC(=O)C(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)CCNC(=O)C(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1021/ml300312b
		49862478	21847	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209458	21847	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		44401585	20535	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL1195347	20535	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL554368	20535	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL264190	217387	1	None	-	2	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm2009937
		10864263	23184	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		CHEMBL12310	23184	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		56679964	70446	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801096	70446	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44577510	195514	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
		CHEMBL504986	195514	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
		71456245	85751	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113039	85751	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423448	92030	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	572	11	0	5	6.2	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCC3)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225968	92030	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	572	11	0	5	6.2	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCC3)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371965	216941	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/jm0614275
		CHEMBL2371969	216945	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0614275
		49862663	21894	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209705	21894	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL438294	220545	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL2370695	216691	0	None	2	2	Mouse	5.3	pIC50	=	5.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		49862378	21814	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209321	21814	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		52943061	24920	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269568	24920	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		44397411	133163	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365074	133163	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		56672278	72691	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	1231	38	16	16	-2.4	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCC(=O)NC(CCCNC(C)=O)(CCCNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835947	72691	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	1231	38	16	16	-2.4	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCC(=O)NC(CCCNC(C)=O)(CCCNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL2331675	216312	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)nn1)C(=O)NCCC(N)=O	10.1021/ml300312b
		16132144	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		16133793	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		44273719	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		CHEMBL214332	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		16132144	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		16133793	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		44273719	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		CHEMBL214332	216058	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		44401530	19567	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188092	19567	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL535152	19567	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44401528	20761	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1196956	20761	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL558787	20761	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		54586246	67591	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1762008	67591	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		145975465	170728	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4207725	170728	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		56683297	70459	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL1801125	70459	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL266288	103738	0	None	-	1	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	5507	70	67	87	-15.6	CSCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CSSSSC[C@@H]3NC(=O)[C@@H]4CCCN4C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](CSSSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(N)=O)NC1=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CSSSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N4)NC3=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSSSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCN=C(N)N)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/jm0303608
		44358625	37973	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	535	11	1	7	5.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NCCOc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL140077	37973	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	535	11	1	7	5.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NCCOc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL524861	222402	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		52940633	24923	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269570	24923	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
		10030530	24371	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125819	24371	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL413226	219835	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		56683296	70453	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801119	70453	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL455070	220778	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		71452716	85668	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2112920	85668	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		6918707	110969	1	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	110969	1	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL1172428	215365	0	None	-	3	Human	6.3	pIC50	=	6.3	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172428	215365	0	None	-	3	Human	6.3	pIC50	=	6.3	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL365794	218820	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371828	216912	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)C(C)=O	10.1021/jm0490033
		CHEMBL2371833	216915	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL3600922	218604	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600843	218599	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		2683	109665	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL305906	109665	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL334255	109665	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL1775066	215660	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1016/j.bmcl.2011.03.019
		44392015	19550	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1187982	19550	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL3216179	19550	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		10004020	25620	2	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12811	25620	2	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44423376	19640	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188733	19640	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL537208	19640	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44441646	160867	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398487	160867	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		49862737	21911	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209789	21911	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44423373	19545	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1187954	19545	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL534503	19545	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		24774521	161037	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL398635	161037	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44448480	102333	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257616	102333	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		56666397	70448	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801098	70448	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		145988152	173823	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4288909	173823	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		49862478	21847	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209458	21847	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		44423464	92181	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(Cl)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226341	92181	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(Cl)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		127047853	146771	0	None	-	0	Mouse	7.3	pIC50	=	7.3	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799955	146771	0	None	-	0	Mouse	7.3	pIC50	=	7.3	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		71459938	85756	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	85756	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2369485	216407	0	None	-	0	Mouse	6.3	pIC50	=	6.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		122184634	129211	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600915	129211	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		56669816	70451	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801117	70451	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		71461652	85755	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113042	85755	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423439	92016	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(Br)c2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225801	92016	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(Br)c2)CC1	10.1016/j.bmc.2006.12.039
		44423421	150108	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389733	150108	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		168295131	199021	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5205283	199021	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44396140	174999	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL433574	174999	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371962	216938	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0614275
		44397633	133158	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365051	133158	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		5624	39467	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL1203324	39467	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL141343	39467	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		11730771	22028	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		CHEMBL12120	22028	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		56659465	70444	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801094	70444	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		145973779	171511	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	929	11	12	9	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4217528	171511	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	929	11	12	9	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3600840	218596	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL389674	219212	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44423420	92198	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226441	92198	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10874535	23293	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		CHEMBL12369	23293	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		11733360	105152	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL275299	105152	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44441642	161184	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398816	161184	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44397220	174083	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL429387	174083	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL413439	219849	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL438920	220588	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401310	19557	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188043	19557	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL534930	19557	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		44448660	101748	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254589	101748	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		49862743	21916	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209794	21916	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL3600833	218593	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		118735100	125578	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421677	125578	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		56676633	70455	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801121	70455	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
		49862738	21912	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209790	21912	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44441684	100906	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL249321	100906	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
		44441633	101305	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL251735	101305	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44457067	104518	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL271586	104518	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		15603023	104740	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL272660	104740	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44397657	130901	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363384	130901	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		16157270	219332	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		CHEMBL405282	219332	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		16157270	219332	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL405282	219332	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL380638	219050	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
		73351850	96294	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2373212	96294	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		127053936	159019	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	598	11	2	4	5.7	O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1	nan
		CHEMBL3968918	159019	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	598	11	2	4	5.7	O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1	nan
		10146211	71103	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL181162	71103	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		489667	66074	1	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	452	8	2	1	7.5	Cc1ccc2[nH]c(-c3ccc(Br)cc3)c(CCCCCNC3CCCCC3)c2c1	10.1021/jm0309452
		CHEMBL170530	66074	1	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	452	8	2	1	7.5	Cc1ccc2[nH]c(-c3ccc(Br)cc3)c(CCCCCNC3CCCCC3)c2c1	10.1021/jm0309452
		168282779	197950	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C	10.1021/acs.jmedchem.1c01848
		CHEMBL5188894	197950	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C	10.1021/acs.jmedchem.1c01848
		49862377	21813	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209320	21813	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		44423469	92203	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	596	10	0	4	6.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226497	92203	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	596	10	0	4	6.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2369775	216465	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		168285801	198260	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
		CHEMBL5193501	198260	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
		44441637	100824	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248892	100824	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL188459	215836	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL1172429	215366	0	None	-	4	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		44441688	101129	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL250719	101129	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		49862375	21811	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209318	21811	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL439691	220627	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44449216	102046	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL256286	102046	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		145980719	173275	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4278563	173275	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL204310	215943	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/jm0510326
		44423451	92085	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	11	0	4	6.2	CC(C)N1CCN(C(CN2CCN(CCCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226072	92085	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	11	0	4	6.2	CC(C)N1CCN(C(CN2CCN(CCCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600835	218595	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44391999	20681	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1196338	20681	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL3215542	20681	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		44423436	92014	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(F)c2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225799	92014	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(F)c2)CC1	10.1016/j.bmc.2006.12.039
		44397652	130412	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361883	130412	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349173	123768	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
		CHEMBL338768	123768	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
		44441686	104019	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL268722	104019	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
		24848934	85727	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113004	85727	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
		155566718	182695	0	None	-3	2	Mouse	5.2	pIC50	=	5.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4587214	182695	0	None	-3	2	Mouse	5.2	pIC50	=	5.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44275312	148185	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL384036	148185	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		44310242	163088	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932912	163088	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL406550	163088	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		71461652	85755	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113042	85755	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		6918813	138149	3	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	138149	3	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL509582	222325	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		49862742	21742	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1208802	21742	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
		1323	9465	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		92432	9465	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		CHEMBL430239	9465	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		132938008	166292	0	None	-	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4102048	166292	0	None	-	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		49862741	21915	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209793	21915	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
		6918707	110969	1	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	110969	1	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		24857886	162027	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402769	162027	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		44408388	147101	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL380635	147101	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44396140	174999	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL433574	174999	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3577981	218528	1	None	-	3	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL3577981	218528	1	None	29	3	Mouse	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		11555886	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL404696	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
		11555886	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL404696	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44397461	133005	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365005	133005	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		11555886	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
		CHEMBL404696	162413	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
		CHEMBL1172429	215366	0	None	-	4	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		1337	10197	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	10197	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	10197	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		56665372	72688	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930592	72688	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835944	72688	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		145967155	171022	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4211275	171022	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3350396	218258	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		22318639	144088	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	10	0	4	5.7	CC(C)N1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL375251	144088	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	10	0	4	5.7	CC(C)N1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371967	216943	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0614275
		10146483	70952	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		CHEMBL180854	70952	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		122184636	129213	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600917	129213	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		56665373	72689	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930593	72689	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835945	72689	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		145973975	171436	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4216654	171436	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3349030	218184	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		10168556	70647	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		CHEMBL180366	70647	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		44310259	168479	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932914	168479	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL413465	168479	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		145966490	171141	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212762	171141	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2371964	216940	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44423435	92012	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	470	9	0	4	4.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225750	92012	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	470	9	0	4	4.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2)CC1	10.1016/j.bmc.2006.12.039
		44397458	74088	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	11	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188404	74088	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	11	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44347838	103418	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1561	33	16	22	-0.6	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		CHEMBL263585	103418	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1561	33	16	22	-0.6	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		44423443	213154	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	6.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(-c3ccccc3)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL87552	213154	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	6.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(-c3ccccc3)cc2)CC1	10.1016/j.bmc.2006.12.039
		44441635	174309	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	492	7	2	4	4.0	CCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL430015	174309	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	492	7	2	4	4.0	CCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44448479	162150	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403420	162150	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		1334	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16133814	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL437050	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL204263	215942	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
		CHEMBL217584	216156	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		1334	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16133814	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		CHEMBL437050	8283	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		24774356	101600	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL253574	101600	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		71456246	85753	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113040	85753	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3601426	218605	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL190551	215845	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190203	215843	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL190427	215844	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL275999	217605	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		44391938	18518	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1181567	18518	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145455	18518	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		6918813	138149	3	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	138149	3	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		1337	10197	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	10197	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	10197	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		44401524	20778	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1197052	20778	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL559181	20778	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44408253	147122	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
		CHEMBL380727	147122	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
		10098971	130802	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	130802	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		155544852	181718	0	None	-1	4	Mouse	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4565367	181718	0	None	-1	4	Mouse	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		46911588	70442	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801092	70442	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44349246	123766	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	12	0	6	4.0	CCCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338766	123766	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	12	0	6	4.0	CCCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		44373177	126609	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL348511	126609	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		1337	10197	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	10197	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	10197	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		145964017	170820	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4208874	170820	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		44448677	162175	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403556	162175	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		44423447	92029	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	13	0	5	6.5	CCC(CC)N1CCN(C(CN2CCN(CCCCc3c(OC)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225967	92029	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	13	0	5	6.5	CCC(CC)N1CCN(C(CN2CCN(CCCCc3c(OC)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10864263	23184	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		CHEMBL12310	23184	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		127046235	146416	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3797690	146416	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		132180597	162950	0	None	-	1	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4063911	162950	0	None	-	1	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		71454492	85730	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113008	85730	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
		145990599	173634	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4285535	173634	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		44441682	161427	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL399474	161427	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL2221249	216222	0	None	-4	3	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O	nan
		CHEMBL4299612	220373	0	None	-	0	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.5b01894
		44423470	92204	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	612	11	0	5	6.7	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(OC(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226498	92204	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	612	11	0	5	6.7	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(OC(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		137653704	165412	0	None	-	1	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4092424	165412	0	None	-	1	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		44391927	20763	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL1196971	20763	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL3216393	20763	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		10117829	92020	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	500	10	0	5	4.8	COc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225856	92020	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	500	10	0	5	4.8	COc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		122184638	129215	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600919	129215	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		56672277	72687	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930591	72687	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835943	72687	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		49862425	21832	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209382	21832	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		46884747	15167	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093306	15167	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397701	132613	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc4ccccc34)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364834	132613	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc4ccccc34)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1338	10579	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		9938402	10579	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		CHEMBL339053	10579	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		44357595	38275	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL140347	38275	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		1324	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16154396	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16197727	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44285019	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		57514683	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		91898441	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		CHEMBL441738	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		DB04931	7090	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		163196518	198908	2	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5203580	198908	2	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		168295644	199091	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5206336	199091	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44349461	23668	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125079	23668	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44349227	125251	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	629	11	0	6	3.6	CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL341316	125251	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	629	11	0	6	3.6	CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3349030	218184	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		52947911	24924	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269571	24924	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		44448588	102096	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL256526	102096	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		127047475	146527	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		132991507	146527	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798421	146527	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44357575	33661	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	604	11	2	6	4.7	O=C(CCNC(=O)c1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL136366	33661	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	604	11	2	6	4.7	O=C(CCNC(=O)c1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		15602927	164661	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL408398	164661	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44426649	159913	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	737	21	10	7	0.4	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2007.04.001
		CHEMBL397652	159913	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	737	21	10	7	0.4	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2007.04.001
		44358622	20434	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1194620	20434	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL553000	20434	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL413260	219838	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		CHEMBL65339	222639	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		44423471	149302	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	571	11	0	5	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(N(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389073	149302	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	571	11	0	5	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(N(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44310243	175966	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932909	175966	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL440633	175966	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		44315095	109910	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	559	13	3	4	4.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL307857	109910	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	559	13	3	4	4.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		137639815	163581	0	None	-	1	Mouse	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4071063	163581	0	None	-	1	Mouse	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		56676634	70458	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL1801124	70458	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		44397355	133929	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365675	133929	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3349030	218184	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		44445084	167518	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	829	9	11	9	0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL411391	167518	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	829	9	11	9	0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44390423	70538	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180157	70538	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL3601431	218606	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		145948876	174262	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL4299441	174262	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
		44397661	130579	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL362314	130579	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358848	125762	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL342470	125762	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL3600912	218600	0	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44358630	35087	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL137452	35087	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL541866	35087	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423380	19857	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1190224	19857	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL540373	19857	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL3600920	218602	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL2371971	216947	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O	10.1021/jm0614275
		1325	10372	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		6440621	10372	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		9898183	10372	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		CHEMBL3422426	10372	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		44366081	17034	0	None	2	2	Human	9.8	pKd	=	9.8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL1161313	17034	0	None	2	2	Human	9.8	pKd	=	9.8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		1325	10372	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		6440621	10372	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		9898183	10372	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL3422426	10372	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL440801	220648	0	None	25	2	Human	9.7	pKd	=	9.7	Binding	pA2 against human melanocortin receptor, human Melanocortin 4 receptorpA2 against human melanocortin receptor, human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303103
		CHEMBL2096742	215985	0	None	5	2	Human	9.3	pKd	=	9.3	Binding	pA2 against human melanocortin receptor, human Melanocortin 4 receptorpA2 against human melanocortin receptor, human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303103
		CHEMBL1161322	215287	0	None	1	2	Human	9.3	pKd	=	9.3	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		122178167	128038	0	None	162	2	Mouse	9.1	pKd	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577996	128038	0	None	162	2	Mouse	9.1	pKd	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL2096742	215985	0	None	5	2	Human	9.1	pKd	=	9.1	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0202526
		CHEMBL1161323	215288	0	None	5	2	Human	8.9	pKd	=	8.9	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O	10.1021/jm0202526
		CHEMBL1161316	215283	0	None	63	2	Human	8.0	pKd	=	8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O	10.1021/jm0202526
		CHEMBL2372589	217052	0	None	-15	2	Human	8.0	pKd	=	8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0202526
		122178155	128029	0	None	-	1	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577985	128029	0	None	-	1	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178158	128031	0	None	10	2	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577987	128031	0	None	10	2	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3422430	218448	0	None	-	1	Mouse	6.0	pKd	=	6	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/ml500340z
		122178161	128033	0	None	-	1	Mouse	5.9	pKd	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577990	128033	0	None	-	1	Mouse	5.9	pKd	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		118735604	125655	0	None	251	2	Mouse	7.8	pKd	=	7.8	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	860	18	10	6	2.0	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		CHEMBL3422427	125655	0	None	251	2	Mouse	7.8	pKd	=	7.8	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	860	18	10	6	2.0	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		122178157	128030	0	None	50	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577986	128030	0	None	50	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178164	128036	0	None	158	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577993	128036	0	None	158	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3422431	218449	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/ml500340z
		CHEMBL3577977	218524	0	None	3	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577980	218527	0	None	7	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577982	218529	0	None	3	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577988	218530	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578001	218534	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577981	218528	1	None	29	3	Mouse	7.7	pKd	=	7.7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161321	215286	0	None	19	2	Human	7.7	pKd	=	7.7	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1021/jm0202526
		CHEMBL2372588	217051	0	None	316	2	Human	8.6	pKd	=	8.6	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O	10.1021/jm0202526
		122178168	128039	0	None	25	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577997	128039	0	None	25	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577995	218531	0	None	6	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578000	218533	0	None	50	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161318	215284	0	None	79	2	Human	8.4	pKd	=	8.4	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O	10.1021/jm0202526
		CHEMBL3577976	218523	0	None	2	2	Mouse	6.5	pKd	=	6.5	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161320	215285	0	None	-12	2	Human	6.5	pKd	=	6.5	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O	10.1021/jm0202526
		118735609	125658	0	None	251	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		CHEMBL3422432	125658	0	None	251	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		118735610	125659	0	None	398	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		CHEMBL3422433	125659	0	None	398	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		122178169	128040	0	None	31	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577998	128040	0	None	31	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577999	218532	0	None	19	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		118735605	125656	0	None	-	1	Mouse	6.3	pKd	=	6.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	897	19	9	6	3.2	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/ml500340z
		CHEMBL3422428	125656	0	None	-	1	Mouse	6.3	pKd	=	6.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	897	19	9	6	3.2	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/ml500340z
		122178162	128034	0	None	-	1	Mouse	8.2	pKd	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577991	128034	0	None	-	1	Mouse	8.2	pKd	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178165	128037	0	None	-	1	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577994	128037	0	None	-	1	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577978	218525	0	None	10	2	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		118735606	125657	0	None	-	1	Mouse	7.1	pKd	=	7.1	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	877	18	9	7	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/ml500340z
		CHEMBL3422429	125657	0	None	-	1	Mouse	7.1	pKd	=	7.1	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	877	18	9	7	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/ml500340z
		162676295	190232	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4798971	190232	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162676295	190232	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4798971	190232	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673931	189837	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794168	189837	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673931	189837	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794168	189837	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673650	189832	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794121	189832	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673650	189832	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794121	189832	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643092	188503	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4777048	188503	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643092	188503	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4777048	188503	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672837	189800	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4793821	189800	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162668987	189369	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4788071	189369	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672837	189800	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4793821	189800	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162668987	189369	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4788071	189369	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672763	189903	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794990	189903	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672763	189903	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794990	189903	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672255	189650	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791788	189650	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672255	189650	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791788	189650	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		1325	10372	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		6440621	10372	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		9898183	10372	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL3422426	10372	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		1325	10372	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		6440621	10372	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		9898183	10372	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL3422426	10372	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		162677133	190336	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4800268	190336	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162677133	190336	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4800268	190336	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643518	188490	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776915	188490	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643518	188490	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776915	188490	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		166585475	198319	0	None	-	1	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	475	5	1	7	3.9	COc1cc(OC)cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5cnn(C)c5)c(C)nc4N3)C2)c1	10.1021/acsmedchemlett.2c00229
		CHEMBL5194472	198319	0	None	-	1	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	475	5	1	7	3.9	COc1cc(OC)cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5cnn(C)c5)c(C)nc4N3)C2)c1	10.1021/acsmedchemlett.2c00229
		1338	10579	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		9938402	10579	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL339053	10579	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL3663320	218831	0	None	9	2	Human	10.3	pKi	=	10.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663321	218832	0	None	3	2	Human	10.3	pKi	=	10.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL442504	220695	0	None	1	3	Human	10.2	pKi	=	10.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		CHEMBL3663336	218845	0	None	-	1	Human	10.2	pKi	=	10.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663319	218830	0	None	3	2	Human	10.1	pKi	=	10.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		57817763	83702	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70690940	83702	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929808	83702	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070251	83702	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL3663337	218846	0	None	-	1	Human	10.1	pKi	=	10.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2C)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL415165	219955	0	None	1	5	Rat	10.1	pKi	=	10.1	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm0501432
		89703076	150968	0	None	-4	2	Human	10.0	pKi	=	10.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3904232	150968	0	None	-4	2	Human	10.0	pKi	=	10.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL385465	219130	0	None	10	3	Human	10.0	pKi	=	10.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		57646437	83697	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684621	83697	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929804	83697	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070246	83697	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		57646441	83695	0	None	13	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070243	83695	0	None	13	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		59149264	83577	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684624	83577	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929810	83577	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2069317	83577	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2415082	217212	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		CHEMBL415661	219977	0	None	21	4	Human	9.9	pKi	=	9.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		122194229	130761	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3629347	130761	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3663331	218842	0	None	5	2	Human	9.8	pKi	=	9.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		57817773	83700	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684623	83700	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929806	83700	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070249	83700	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		59149266	83701	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70693081	83701	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929807	83701	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070250	83701	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		57817730	83698	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684622	83698	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929805	83698	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070247	83698	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		166585425	197412	0	None	-	1	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5181223	197412	0	None	-	1	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL2370968	216750	0	None	-1	3	Human	9.7	pKi	=	9.7	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		CHEMBL3663327	218838	0	None	1	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663332	218843	0	None	-1	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1ccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)cc1	nan
		CHEMBL3663370	218878	0	None	2	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		10408	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		5329	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		9941379	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		CHEMBL2070241	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		DB11653	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		166585537	197282	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	478	4	1	7	4.0	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5179337	197282	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	478	4	1	7	4.0	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		44347220	175219	0	None	112	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	861	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL434985	175219	0	None	112	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	861	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		59149255	83703	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70693082	83703	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929809	83703	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070252	83703	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL414718	219930	0	None	-3	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
		CHEMBL331259	218140	0	None	70	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O	10.1021/jm010165y
		166585598	196922	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	517	4	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc6ccccn6n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5173560	196922	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	517	4	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc6ccccn6n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL407809	219464	0	None	35	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL3663342	218851	0	None	-	1	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663363	218872	0	None	83	2	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		1324	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		16154396	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		16197727	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		44285019	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		57514683	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		91898441	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		CHEMBL441738	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		DB04931	7090	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		CHEMBL412523	219779	0	None	22	4	Human	9.5	pKi	=	9.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL415165	219955	0	None	-3	5	Human	9.5	pKi	=	9.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		70688853	83699	0	None	9	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070248	83699	0	None	9	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL3663378	218886	0	None	34	2	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H]([C@@H](C)OCc2ccccc2)NC1=O	nan
		44347119	121200	0	None	151	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	752	9	10	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333178	121200	0	None	151	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	752	9	10	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		57646411	83696	0	None	1	4	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070245	83696	0	None	1	4	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL267900	217516	0	None	1	4	Rat	9.4	pKi	=	9.4	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44415919	148366	0	None	2	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL385000	148366	0	None	2	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88590706	132304	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646867	132304	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646851	218775	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590706	132304	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646867	132304	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646851	218775	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88287852	134337	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1044	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663335	134337	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1044	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CCN)NC1=O	nan
		166585402	196723	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	531	5	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc(C(F)F)n(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5170290	196723	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	531	5	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc(C(F)F)n(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		1324	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16154396	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16197727	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44285019	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		57514683	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		91898441	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		CHEMBL441738	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		DB04931	7090	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		166585467	197010	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	480	5	1	7	4.0	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)[C@@H](C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5174952	197010	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	480	5	1	7	4.0	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)[C@@H](C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL408257	219483	0	None	23	3	Human	9.4	pKi	=	9.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL3663340	218849	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](CCN)NC1=O	nan
		1323	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		92432	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL430239	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		1323	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		92432	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL430239	9465	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		162670951	189617	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791306	189617	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162670951	189617	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791306	189617	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		164889476	197573	4	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	462	4	1	7	3.5	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5183637	197573	4	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	462	4	1	7	3.5	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1	10.1021/acsmedchemlett.2c00229
		1324	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16154396	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16197727	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44285019	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		57514683	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		91898441	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		CHEMBL441738	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		DB04931	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44347219	23352	0	None	301	3	Human	9.3	pKi	=	9.3	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	781	9	10	8	0.2	NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		CHEMBL123938	23352	0	None	301	3	Human	9.3	pKi	=	9.3	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	781	9	10	8	0.2	NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		CHEMBL3663334	218844	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663345	218854	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667945	218918	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		44443035	161196	0	None	-26	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	161196	0	None	-26	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL264352	217396	0	None	1	4	Rat	9.3	pKi	=	9.3	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL2373515	217158	0	None	1	3	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		166585443	197056	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		CHEMBL5175663	197056	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		168288063	198416	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	514	5	1	7	4.6	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3cc(OC(F)F)ncc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5195837	198416	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	514	5	1	7	4.6	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3cc(OC(F)F)ncc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		162672691	189980	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4795842	189980	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL266879	217485	0	None	-2	4	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0501432
		CHEMBL267900	217516	0	None	-1	4	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		162672691	189980	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4795842	189980	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		1324	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL408843	219514	0	None	-1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		1324	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44347331	23099	0	None	181	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL122773	23099	0	None	181	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		44410040	83293	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL205996	83293	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL2070374	215966	0	None	22	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		24740655	95861	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL236521	95861	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
		44415914	146048	0	None	1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL379054	146048	0	None	1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44443035	161196	0	None	26	4	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	161196	0	None	26	4	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL3644324	218743	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644324	218743	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663329	218840	0	None	5	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663367	218875	0	None	5	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663368	218876	0	None	10	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		23635109	98334	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635109	98334	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL240572	98334	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240572	98334	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		24740655	95861	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		CHEMBL236521	95861	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		1324	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		1324	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		1324	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL3663372	218880	0	None	1	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663343	218852	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644293	218716	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644348	218766	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		134143749	157391	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1133	19	15	12	3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3955282	157391	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1133	19	15	12	3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644348	218766	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3663325	218836	0	None	1	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663339	218848	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc([N+](=O)[O-])c2)NC(=O)[C@H](CCN)NC1=O	nan
		44433290	103236	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	10	2	5	4.7	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)[C@@H](C)N)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL262321	103236	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	10	2	5	4.7	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)[C@@H](C)N)c1	10.1016/j.bmcl.2007.07.097
		24180646	154961	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	154961	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180646	154961	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL393576	154961	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL267492	217503	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		CHEMBL3663318	218829	0	None	1	2	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667943	218916	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667944	218917	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88944291	160129	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3978439	160129	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL1923665	215866	0	None	1	3	Human	9.1	pKi	=	9.1	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm201226w
		162643435	188446	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776340	188446	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL1923667	215867	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm201226w
		CHEMBL264352	217396	0	None	-1	4	Human	9.1	pKi	=	9.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		162643435	188446	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776340	188446	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		122178167	128038	0	None	162	2	Mouse	9.1	pKi	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577996	128038	0	None	162	2	Mouse	9.1	pKi	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44415913	86726	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL212614	86726	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88590696	132305	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646868	132305	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590696	132305	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646868	132305	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		44434550	95304	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	641	9	3	5	5.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCNCC2)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL235190	95304	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	641	9	3	5	5.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCNCC2)CC1	10.1016/j.bmc.2007.05.026
		44434562	95473	0	None	301	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236014	95473	0	None	301	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44577093	185425	0	None	42	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL467587	185425	0	None	42	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		1324	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		10325306	148042	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL383117	148042	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL3663323	218834	0	None	6	2	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL268851	217548	0	None	33	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		44347221	23407	0	None	53	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL124169	23407	0	None	53	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44432941	94338	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233559	94338	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24180593	155222	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393788	155222	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL3667940	218913	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44432941	94338	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233559	94338	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24180646	154961	0	None	-1	8	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL393576	154961	0	None	-1	8	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		168277761	197079	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2342	37	34	29	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5175981	197079	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2342	37	34	29	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		162665450	189075	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4784053	189075	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162665450	189075	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4784053	189075	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL267492	217503	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		24180646	154961	0	None	-1	8	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	154961	0	None	-1	8	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433276	96450	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.9	CC(C)C[C@H](NCCCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237578	96450	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.9	CC(C)C[C@H](NCCCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		1324	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		16154396	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		16197727	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		44285019	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		57514683	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		91898441	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		CHEMBL441738	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		DB04931	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		CHEMBL3663330	218841	0	None	9	2	Human	9.0	pKi	=	9.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C(F)(F)F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663369	218877	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44432966	153079	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL392092	153079	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432966	153079	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL392092	153079	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		1324	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44433270	95858	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	641	11	2	5	5.5	CC(C)C[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236519	95858	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	641	11	2	5	5.5	CC(C)C[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433287	168045	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	11	2	5	4.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL412023	168045	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	11	2	5	4.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180646	154961	0	None	-1	8	Rat	9.0	pKi	=	9	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	154961	0	None	-1	8	Rat	9.0	pKi	=	9	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10257541	133120	0	None	123	4	Human	9.0	pKi	=	9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL365039	133120	0	None	123	4	Human	9.0	pKi	=	9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		88212540	131844	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644356	131844	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		89007953	158409	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3963781	158409	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644316	218735	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646856	218779	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590676	132306	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646869	132306	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644292	218715	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)OCc2ccccc2)NC1=O	nan
		88212540	131844	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644356	131844	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590676	132306	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646869	132306	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134153366	159574	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1121	20	16	12	3.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)OCc2ccccc2)/N=C\1O	nan
		CHEMBL3973691	159574	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1121	20	16	12	3.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)OCc2ccccc2)/N=C\1O	nan
		90684343	166962	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1069	18	17	11	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL4109346	166962	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1069	18	17	11	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL3644316	218735	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646856	218779	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663349	218858	0	None	144	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663366	218874	0	None	1	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663375	218883	0	None	89	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667939	218912	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667947	218920	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL2070244	215963	0	None	4	4	Human	9.0	pKi	=	9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44434548	155129	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL393716	155129	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44456222	104701	0	None	223	3	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272538	104701	0	None	223	3	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44456102	162383	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL404549	162383	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL2370154	216580	0	None	1	3	Human	9.0	pKi	=	9	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm020021z
		44433296	159824	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	669	11	2	5	5.4	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397581	159824	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	669	11	2	5	5.4	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416057	87966	0	None	1	3	Human	9.0	pKi	=	9.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215833	87966	0	None	1	3	Human	9.0	pKi	=	9.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44577092	185424	0	None	11	3	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467586	185424	0	None	11	3	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		25022598	101805	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL255007	101805	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		1324	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		11017471	38691	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm049278i
		CHEMBL140738	38691	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm049278i
		CHEMBL412495	219777	0	None	12	3	Human	8.9	pKi	=	8.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		1323	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		92432	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		CHEMBL430239	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		1323	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		92432	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL430239	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		1323	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		92432	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		CHEMBL430239	9465	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		44400814	77396	0	None	446	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	627	11	3	5	5.9	O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194990	77396	0	None	446	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	627	11	3	5	5.9	O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44415920	87146	0	None	3	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL214410	87146	0	None	3	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44416106	148224	0	None	5	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL384176	148224	0	None	5	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44577095	185533	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	9	2	5	4.6	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL468636	185533	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	9	2	5	4.6	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL267492	217503	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		1324	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		162669632	189344	0	None	6	2	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4787753	189344	0	None	6	2	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		44433298	159826	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397583	159826	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433277	175705	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	655	12	2	5	5.9	CC(C)C[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL438683	175705	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	655	12	2	5	5.9	CC(C)C[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400810	130838	0	None	316	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	11	3	5	5.4	CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL363190	130838	0	None	316	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	11	3	5	5.4	CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44456222	104701	0	None	223	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272538	104701	0	None	223	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		25131478	176287	0	None	44	3	Human	8.9	pKi	=	8.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL443396	176287	0	None	44	3	Human	8.9	pKi	=	8.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL2370963	216745	0	None	10	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44347331	23099	0	None	181	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL122773	23099	0	None	181	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL2370553	216649	0	None	10	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		44433271	96314	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
		CHEMBL237365	96314	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
		44433299	159827	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397584	159827	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400935	77637	0	None	104	4	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	10	2	5	5.5	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195110	77637	0	None	104	4	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	10	2	5	5.5	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415084	217214	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(N)=O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		CHEMBL267492	217503	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		CHEMBL420167	220021	0	None	8	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		44412933	83398	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	611	13	3	6	4.1	COc1ccccc1CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL206364	83398	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	611	13	3	6	4.1	COc1ccccc1CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44400864	131103	0	None	177	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	11	3	5	5.0	CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL363576	131103	0	None	177	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	11	3	5	5.0	CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562476	192794	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487044	192794	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415081	217211	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		56851058	75848	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		57394091	75848	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		91930626	75848	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL1923666	75848	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL267492	217503	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432950	93566	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232162	93566	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432950	93566	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232162	93566	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		6918814	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL365597	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		6918814	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL365597	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415019	217209	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCCc1cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44434546	95574	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236423	95574	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44434547	95575	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236424	95575	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		6918814	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL365597	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		6918814	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL365597	133835	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44443033	100473	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL247010	100473	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
		44433294	159822	0	None	575	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397580	159822	0	None	575	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10077773	94042	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233135	94042	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44409103	146901	0	None	-1	3	Human	8.0	pKi	=	8	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
		CHEMBL380120	146901	0	None	-1	3	Human	8.0	pKi	=	8	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
		44391382	137232	0	None	-	1	Human	8.0	pKi	=	8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	9	4	6	4.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL368023	137232	0	None	-	1	Human	8.0	pKi	=	8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	9	4	6	4.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3663351	218860	0	None	81	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663361	218870	0	None	1000	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3667925	218898	0	None	39	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667928	218901	0	None	21	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44434549	95941	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236625	95941	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		16038316	86531	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	583	11	2	6	4.1	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211742	86531	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	583	11	2	6	4.1	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		44444509	100743	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248435	100743	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447250	101502	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL253028	101502	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44577090	185445	0	None	57	3	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467771	185445	0	None	57	3	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		46885482	15102	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092860	15102	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		11845272	87133	0	None	4	3	Human	8.0	pKi	=	8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL214347	87133	0	None	4	3	Human	8.0	pKi	=	8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		44412510	145179	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	635	11	2	6	4.6	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CN2CCOCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377313	145179	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	635	11	2	6	4.6	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CN2CCOCC2)CC1	10.1016/j.bmcl.2006.04.002
		44412613	145704	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378411	145704	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL5090670	222056	0	None	1	3	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44410803	146950	0	None	87	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380365	146950	0	None	87	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL5090285	222032	0	None	-3	3	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11181804	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL366706	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		44323034	213309	0	None	-2	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88537	213309	0	None	-2	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44323032	213383	0	None	-5	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL89004	213383	0	None	-5	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL3644311	218730	0	None	-	1	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644311	218730	0	None	-	1	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944278	156319	0	None	-6606	2	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	967	19	13	10	-0.2	CCCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3946641	156319	0	None	-6606	2	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	967	19	13	10	-0.2	CCCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		122178155	128029	0	None	-	1	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577985	128029	0	None	-	1	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178158	128031	0	None	10	2	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577987	128031	0	None	10	2	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433409	158993	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	9	1	4	6.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396868	158993	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	9	1	4	6.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44405450	79293	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199061	79293	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44405364	79297	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	10	2	5	4.5	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccco3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199073	79297	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	10	2	5	4.5	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccco3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447224	161479	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	9	2	6	4.6	CN[C@H](C)C(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399762	161479	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	9	2	6	4.6	CN[C@H](C)C(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44442992	100698	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	1	5	5.0	COCC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248206	100698	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	1	5	5.0	COCC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443004	101263	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.7	CNCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251495	101263	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.7	CNCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404576	78727	0	None	-	1	Human	7.0	pKi	=	7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1ccc(F)cc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197288	78727	0	None	-	1	Human	7.0	pKi	=	7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1ccc(F)cc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44413684	18590	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182072	18590	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL209417	18590	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		44393418	162479	0	None	3	4	Human	6.0	pKi	=	6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL405150	162479	0	None	3	4	Human	6.0	pKi	=	6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44395572	73214	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	467	9	1	4	5.0	O=C(CCc1ccc(Cl)cc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL185200	73214	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	467	9	1	4	5.0	O=C(CCc1ccc(Cl)cc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44395464	73750	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccccc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186794	73750	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccccc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44405563	79225	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	12	2	4	5.0	CCC(CC)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198837	79225	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	12	2	4	5.0	CCC(CC)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44412680	85606	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211280	85606	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		44412690	86227	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	4	6	3.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211366	86227	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	4	6	3.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44415430	86738	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	9	1	4	5.6	NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212653	86738	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	9	1	4	5.6	NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44432885	93772	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232388	93772	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		70685981	81849	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	351	7	3	3	1.5	O=C(NCCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035936	81849	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	351	7	3	3	1.5	O=C(NCCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		70683848	81860	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	540	12	2	5	3.4	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCOc2ccccc2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035947	81860	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	540	12	2	5	3.4	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCOc2ccccc2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL263878	217377	0	None	-45	3	Human	5.0	pKi	=	5	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		88944295	149753	0	None	-1122	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	910	15	11	10	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3894392	149753	0	None	-1122	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	910	15	11	10	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660698	150051	0	None	-288	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3896855	150051	0	None	-288	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660688	150476	0	None	-4	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	783	13	10	9	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3900322	150476	0	None	-4	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	783	13	10	9	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		68342929	154392	0	None	-32	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	825	13	12	9	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3931237	154392	0	None	-32	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	825	13	12	9	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		88944294	154709	0	None	-12589	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	15	11	10	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3933740	154709	0	None	-12589	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	15	11	10	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660676	155159	0	None	-562	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3937437	155159	0	None	-562	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCCN)NC1=O	nan
		70660680	155833	0	None	-251	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	836	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3942841	155833	0	None	-251	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	836	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660654	156933	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	830	17	12	11	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3951584	156933	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	830	17	12	11	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660696	157517	0	None	-1	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	667	11	8	8	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3956317	157517	0	None	-1	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	667	11	8	8	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660690	158269	0	None	-331	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3962394	158269	0	None	-331	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		70660691	158369	0	None	-3311	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	814	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3963435	158369	0	None	-3311	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	814	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88878681	158495	0	None	-6760	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3964400	158495	0	None	-6760	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660651	158665	0	None	-15	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	738	11	9	9	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3965807	158665	0	None	-15	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	738	11	9	9	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660679	159798	0	None	-501	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3975629	159798	0	None	-501	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88878668	161064	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3986527	161064	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660695	161089	0	None	-1412	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	823	15	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3986675	161089	0	None	-1412	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	823	15	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434621	153083	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	561	9	1	5	6.4	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL392094	153083	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	561	9	1	5	6.4	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		44434581	173830	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	7	2	2	5.2	NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL428903	173830	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	7	2	2	5.2	NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		11845440	145450	0	None	-8	3	Human	6.0	pKi	=	6.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
		CHEMBL377778	145450	0	None	-8	3	Human	6.0	pKi	=	6.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
		44393877	129031	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL359777	129031	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		168283887	197799	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186784	197799	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		11851038	147113	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44409240	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
		CHEMBL202699	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
		44409240	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		CHEMBL202699	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		44409240	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
		CHEMBL202699	81209	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
		44432885	93772	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232388	93772	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44401386	76299	0	None	2	2	Human	6.0	pKi	=	6.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	593	12	6	4	3.6	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL193409	76299	0	None	2	2	Human	6.0	pKi	=	6.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	593	12	6	4	3.6	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1	10.1016/j.bmcl.2005.03.120
		44404544	78895	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(C)=O	10.1016/j.bmcl.2005.08.018
		CHEMBL197820	78895	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(C)=O	10.1016/j.bmcl.2005.08.018
		46203215	15242	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1093856	15242	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1204065	15242	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		10304794	146183	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	146183	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44401587	17073	0	None	-1	2	Human	5.0	pKi	=	5.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	611	15	6	5	2.6	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161794	17073	0	None	-1	2	Human	5.0	pKi	=	5.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	611	15	6	5	2.6	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44401367	168498	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL413565	168498	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		168293053	198845	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5202611	198845	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432927	94175	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL233357	94175	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL3667954	218927	0	None	9	2	Human	6.0	pKi	=	6.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(=O)O)NC1=O	nan
		10481883	84110	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL208376	84110	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		11181804	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		CHEMBL366706	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		44562558	180932	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCCC(C)(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454663	180932	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCCC(C)(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562559	195739	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508285	195739	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44416135	86959	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL213566	86959	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
		11181804	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL366706	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL3663338	218847	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2[N+](=O)[O-])NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663348	218857	0	None	48	2	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL3663371	218879	0	None	2	2	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC1=O	nan
		CHEMBL2331674	216311	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		44393887	73448	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185417	73448	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		11181804	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL366706	135285	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		23661656	175823	0	None	-1	5	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	175823	0	None	-1	5	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		24873537	152839	0	None	20	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL391902	152839	0	None	20	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44405360	140339	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371063	140339	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44444497	161791	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL401465	161791	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		44447785	101852	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255313	101852	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447777	162194	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403675	162194	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442965	156438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
		CHEMBL394744	156438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
		44443031	161335	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399112	161335	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44416135	86959	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL213566	86959	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
		25133208	178773	0	None	13	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
		CHEMBL447117	178773	0	None	13	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
		44397281	133322	0	None	109	3	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	12	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365237	133322	0	None	109	3	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	12	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44432903	93968	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232724	93968	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44347105	120123	0	None	13	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	724	9	10	7	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL331728	120123	0	None	13	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	724	9	10	7	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44410378	83401	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
		CHEMBL206367	83401	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
		44562368	182526	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	8	2	5	4.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)N2CCCC2=O)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL458329	182526	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	8	2	5	4.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)N2CCCC2=O)CC1	10.1016/j.bmcl.2008.07.076
		44562424	185993	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	2	5	4.3	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL472553	185993	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	2	5	4.3	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44562498	193512	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488719	193512	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562361	195458	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	643	12	0	6	7.0	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL503909	195458	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	643	12	0	6	7.0	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		44322923	213325	0	None	-1	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88630	213325	0	None	-1	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391289	72340	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	700	12	3	8	3.8	CCOC(=O)C1CCN(CNCc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183114	72340	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	700	12	3	8	3.8	CCOC(=O)C1CCN(CNCc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		44391262	135286	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	645	14	3	6	4.6	CC(C)COCCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL366708	135286	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	645	14	3	6	4.6	CC(C)COCCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396114	131129	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	3	6	4.0	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL363688	131129	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	3	6	4.0	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		10325955	172050	0	None	6	4	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL423101	172050	0	None	6	4	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		117723618	157617	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1087	20	18	13	-4.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		CHEMBL3957057	157617	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1087	20	18	13	-4.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		CHEMBL3644342	218761	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		88944178	153259	0	None	-4365	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	953	18	13	10	-0.5	CCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3922330	153259	0	None	-4365	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	953	18	13	10	-0.5	CCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88878681	158495	0	None	-6760	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3964400	158495	0	None	-6760	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44433389	161490	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.2	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL399802	161490	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.2	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44415674	86896	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213264	86896	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415417	86921	0	None	10	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213380	86921	0	None	10	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405613	141002	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	9	2	4	3.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371683	141002	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	9	2	4	3.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447236	161585	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.9	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2CC(=O)OC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400274	161585	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.9	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2CC(=O)OC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44432927	94175	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL233357	94175	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44447770	102437	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL258035	102437	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44447776	168670	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL415094	168670	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443036	100662	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	9	0	5	5.8	COc1ccc(CN(C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL248048	100662	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	9	0	5	5.8	COc1ccc(CN(C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44443018	161088	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	620	9	1	5	6.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4OC(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398667	161088	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	620	9	1	5	6.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4OC(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443006	161945	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.9	NCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL402266	161945	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.9	NCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404563	77098	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	317	9	0	3	3.0	CCN(CC)CC(CCCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL194464	77098	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	317	9	0	3	3.0	CCN(CC)CC(CCCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44397123	134338	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	616	12	3	6	4.1	CN(C)c1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL366334	134338	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	616	12	3	6	4.1	CN(C)c1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44400825	131101	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	638	12	2	7	6.5	O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL363561	131101	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	638	12	2	7	6.5	O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		11295536	64314	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL166328	64314	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		11364802	172068	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL423250	172068	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44412687	86210	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	10	4	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211364	86210	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	10	4	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44444430	101097	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	440	5	1	4	3.6	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250575	101097	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	440	5	1	4	3.6	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44444442	161429	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	0	4	6.2	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)CC(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL399487	161429	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	0	4	6.2	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)CC(C)C	10.1016/j.bmcl.2007.06.088
		44447246	162295	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL404206	162295	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415925	87881	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	523	8	1	4	6.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CC(C)C(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215609	87881	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	523	8	1	4	6.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CC(C)C(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44434611	95389	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	373	6	2	2	3.9	NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL235627	95389	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	373	6	2	2	3.9	NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		10270570	95808	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	6	2	2	4.4	CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236450	95808	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	6	2	2	4.4	CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434850	95949	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL236645	95949	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434683	96078	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	10	3	3	4.9	C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		CHEMBL236847	96078	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	10	3	3	4.9	C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		44434859	96809	0	None	-6	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL238158	96809	0	None	-6	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1	10.1016/j.bmc.2007.06.003
		44432895	93715	1	None	-	1	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL232327	93715	1	None	-	1	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		168293053	198845	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5202611	198845	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL438596	220560	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44404550	79335	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199192	79335	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11851038	147113	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL3644337	218756	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644337	218756	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		11851038	147113	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		46885972	14891	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL1091631	14891	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL5075712	221173	0	None	-77	3	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137659790	166101	0	None	-5	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4099889	166101	0	None	-5	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		89007938	151172	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1059	19	17	12	-3.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3906011	151172	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1059	19	17	12	-3.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644299	218721	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44444429	101096	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	439	5	0	4	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250573	101096	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	439	5	0	4	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		16132144	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		168273045	197033	0	None	1	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	62	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5175392	197033	0	None	1	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	62	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168285101	198423	0	None	-16	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5195937	198423	0	None	-16	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44432895	93715	1	None	-	1	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL232327	93715	1	None	-	1	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		4189	213701	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	213701	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	213701	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL409049	219524	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C	10.1021/jm030119t
		44433300	158212	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	12	2	5	5.0	CC(C)C[C@H](NC(=O)CCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396186	158212	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	12	2	5	5.0	CC(C)C[C@H](NC(=O)CCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11181804	135285	0	None	21	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.08.055
		CHEMBL366706	135285	0	None	21	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644332	218751	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644295	218717	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644310	218729	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644332	218751	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44393888	133860	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL365636	133860	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44433423	95499	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL236110	95499	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44433428	96102	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)C3CN(C4CCOCC4)CC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL236910	96102	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)C3CN(C4CCOCC4)CC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		24873537	152839	0	None	20	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL391902	152839	0	None	20	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44433423	95499	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL236110	95499	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		44412897	146010	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378866	146010	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44416213	86996	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213721	86996	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44432903	93968	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232724	93968	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44447791	162096	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL403047	162096	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443014	160789	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398409	160789	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133210	176236	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
		CHEMBL442829	176236	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
		44397283	73940	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187659	73940	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397304	133604	0	None	158	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365465	133604	0	None	158	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412509	146955	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	12	3	5	5.4	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CNC2CCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL380391	146955	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	12	3	5	5.4	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CNC2CCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		168281681	197534	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5182977	197534	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		168289584	198565	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3108	98	37	41	-6.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198158	198565	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3108	98	37	41	-6.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		24886260	19071	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184895	19071	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL376999	19071	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		9851816	18594	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182091	18594	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211260	18594	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		44433274	158483	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	12	1	5	5.3	CC(C)C[C@H](NCCN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396431	158483	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	12	1	5	5.3	CC(C)C[C@H](NCCN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44562400	181963	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL457059	181963	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44322959	162854	0	None	-5	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL406276	162854	0	None	-5	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391271	70623	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	644	11	3	7	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL180304	70623	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	644	11	3	7	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44391381	72344	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.2	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)C2CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183134	72344	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.2	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)C2CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		44396079	134072	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	562	11	4	6	3.5	CC(NCc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL365874	134072	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	562	11	4	6	3.5	CC(NCc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44393809	72952	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL184325	72952	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433385	95830	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236489	95830	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405377	78799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197541	78799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447245	101449	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL252622	101449	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44447214	175809	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	555	6	1	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL439427	175809	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	555	6	1	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416228	86780	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212802	86780	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44415984	87292	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL214799	87292	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		9842665	163585	12	None	-3	2	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44447778	162195	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403676	162195	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44396953	73657	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	3	7	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL186370	73657	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	3	7	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL427629	220136	0	None	-5	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44562413	181961	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	12	1	4	6.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC(C)C)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL457058	181961	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	12	1	4	6.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC(C)C)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44412864	86469	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	3	7	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Oc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211540	86469	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	3	7	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Oc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		44444441	100801	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	0	4	5.0	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248767	100801	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	0	4	5.0	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44412791	145587	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	3	7	1.4	COCC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378105	145587	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	3	7	1.4	COCC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44444440	161910	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	468	6	0	4	4.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL402059	161910	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	468	6	0	4	4.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44434855	96805	0	None	-2	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	96805	0	None	-2	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44442899	100474	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	446	5	1	4	3.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247045	100474	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	446	5	1	4	3.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44442985	100542	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	589	8	1	5	5.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cc5ccccc5n4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247411	100542	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	589	8	1	5	5.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cc5ccccc5n4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10180932	96182	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	11	2	2	5.8	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237051	96182	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	11	2	2	5.8	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10159196	96513	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	11	2	4	4.4	NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237694	96513	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	11	2	4	4.4	NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434780	154951	0	None	-2	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	525	8	2	2	7.3	NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393568	154951	0	None	-2	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	525	8	2	2	7.3	NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44413829	84841	0	None	1	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL210011	84841	0	None	1	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		168288992	198549	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197875	198549	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		70660697	158814	0	None	-616	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3967140	158814	0	None	-616	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44415956	148734	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
		CHEMBL387246	148734	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
		44415956	148734	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL387246	148734	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		168288992	198549	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197875	198549	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44404545	79072	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC)C(=O)C(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198319	79072	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC)C(=O)C(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11851038	147113	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44393808	72905	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL184068	72905	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL3667953	218926	0	None	77	2	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(=O)O)NC1=O	nan
		44432900	93967	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232723	93967	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		168274920	197042	0	None	-11	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5175444	197042	0	None	-11	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		1338	10579	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44409104	83300	0	None	2	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		CHEMBL206033	83300	0	None	2	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		44410175	175771	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL439158	175771	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
		44562439	185819	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471339	185819	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562286	195769	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CNC)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508641	195769	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CNC)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644299	218721	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646873	218791	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646884	218801	0	None	53	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644299	218721	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646873	218791	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646884	218801	0	None	53	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667927	218900	0	None	776	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44393864	72970	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL184405	72970	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		11786860	73108	1	None	45	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185035	73108	1	None	45	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		16007285	87897	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215659	87897	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444500	100919	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249370	100919	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44444483	162436	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	524	7	0	4	5.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL404854	162436	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	524	7	0	4	5.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.06.088
		44397283	73940	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187659	73940	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412641	84797	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	12	2	5	4.9	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209825	84797	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	12	2	5	4.9	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		44412640	146341	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.9	CCN(CC)CC(C1CCCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379719	146341	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.9	CCN(CC)CC(C1CCCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL427666	220143	0	None	-4	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O	10.1021/jm0501432
		168281969	198057	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190661	198057	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5083551	221648	0	None	-14	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44405368	78737	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197328	78737	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44405582	79245	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	10	2	4	4.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198916	79245	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	10	2	4	4.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447209	101351	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	638	10	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251966	101351	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	638	10	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447211	101354	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	8	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251983	101354	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	8	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412884	146226	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	11	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379400	146226	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	11	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		16132144	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44432900	93967	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232723	93967	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		44447787	162049	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402838	162049	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442944	100375	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL246606	100375	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443024	100897	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(C(F)(F)F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249268	100897	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(C(F)(F)F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404562	78199	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	303	8	0	3	2.6	CCN(CC)CC(CCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL195998	78199	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	303	8	0	3	2.6	CCN(CC)CC(CCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL2370965	216747	0	None	1	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44347081	175406	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL436169	175406	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		11237444	134243	0	None	-245	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
		CHEMBL366042	134243	0	None	-245	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
		11214733	127074	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352677	127074	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		46930942	75178	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	782	24	10	8	1.5	[N-]=[N+]=NCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2011.08.053
		CHEMBL1917057	75178	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	782	24	10	8	1.5	[N-]=[N+]=NCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2011.08.053
		122178161	128033	0	None	-	1	Mouse	5.9	pKi	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577990	128033	0	None	-	1	Mouse	5.9	pKi	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44412881	83805	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	563	10	4	6	2.3	CC(C)NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL207166	83805	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	563	10	4	6	2.3	CC(C)NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44412688	144974	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	627	11	4	7	3.4	COc1ccccc1NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL376974	144974	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	627	11	4	7	3.4	COc1ccccc1NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44434758	95469	0	None	-1	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	755	14	3	5	9.6	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL236002	95469	0	None	-1	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	755	14	3	5	9.6	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44443040	100425	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	0	6	5.7	COc1ccc(CN(CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)OC)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL246807	100425	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	0	6	5.7	COc1ccc(CN(CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)OC)cc1	10.1016/j.bmcl.2007.10.032
		44443042	100701	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	0	5	5.5	CCN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248224	100701	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	0	5	5.5	CCN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347750	23187	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	7	0	3	6.2	CCCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL123113	23187	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	7	0	3	6.2	CCCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		10157774	96076	0	None	-8	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236842	96076	0	None	-8	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434657	97009	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL238341	97009	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		168272746	197303	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5179536	197303	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		176	7186	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	7186	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	7186	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	7186	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	7186	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		88944286	149809	0	None	-660	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	981	19	14	11	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3894840	149809	0	None	-660	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	981	19	14	11	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		168283887	197799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186784	197799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		168276817	196877	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5172843	196877	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		2247	7293	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	7293	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	7293	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	7293	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	7293	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		16132144	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		11845276	86828	0	None	2	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
		CHEMBL212976	86828	0	None	2	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
		CHEMBL438596	220560	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		11847312	86537	0	None	-2	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		CHEMBL211798	86537	0	None	-2	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		168276817	196877	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5172843	196877	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44401440	76895	0	None	1	2	Human	6.9	pKi	=	6.9	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL194011	76895	0	None	1	2	Human	6.9	pKi	=	6.9	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL5091236	222078	0	None	-173	3	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44400711	77887	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	594	11	2	6	4.2	CS(=O)(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195414	77887	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	594	11	2	6	4.2	CS(=O)(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410379	147981	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
		CHEMBL382833	147981	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
		44395681	73644	0	None	70	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	13	3	6	3.8	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186289	73644	0	None	70	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	13	3	6	3.8	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644325	218744	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644325	218744	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		168281681	197534	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5182977	197534	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		44394080	133544	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL365279	133544	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		24741624	145158	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL377231	145158	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL267492	217503	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432953	155420	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393948	155420	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		24741624	145158	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
		CHEMBL377231	145158	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
		11847001	87003	0	None	138	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL213747	87003	0	None	138	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		25132864	179381	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
		CHEMBL449050	179381	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
		25129108	179475	0	None	15	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
		CHEMBL450236	179475	0	None	15	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
		44404549	147296	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL381015	147296	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11157584	175023	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL433710	175023	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.08.018
		44412626	86710	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	10	1	4	5.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)N2CCc3ccccc3C2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL212535	86710	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	10	1	4	5.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)N2CCc3ccccc3C2)CC1	10.1016/j.bmcl.2006.04.002
		44432953	155420	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393948	155420	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44416375	87851	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL215481	87851	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44433278	155226	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	2	5	4.2	CC(C)C[C@H](NCC(N)=O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393789	155226	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	2	5	4.2	CC(C)C[C@H](NCC(N)=O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44322977	118346	0	None	-2	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL328117	118346	0	None	-2	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391303	72091	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	631	11	2	7	3.4	CCOC(=O)CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182900	72091	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	631	11	2	7	3.4	CCOC(=O)CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396102	73507	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	537	11	3	6	3.5	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL185725	73507	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	537	11	3	6	3.5	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44395920	103574	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	581	13	3	6	4.4	CCC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL264983	103574	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	581	13	3	6	4.4	CCC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		11753667	63952	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164857	63952	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644301	218723	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		134143956	157331	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	17	17	12	1.5	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)O)/N=C\1O	nan
		CHEMBL3954833	157331	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	17	17	12	1.5	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)O)/N=C\1O	nan
		44405549	78657	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	578	10	2	4	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197075	78657	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	578	10	2	4	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44415433	88007	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215851	88007	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405378	147343	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		CHEMBL381197	147343	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		44416375	87851	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215481	87851	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44442990	100481	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	4	6.2	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL247088	100481	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	4	6.2	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44443017	160920	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4C(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398542	160920	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4C(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44347765	23540	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	5	0	3	5.3	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)c(C)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL124410	23540	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	5	0	3	5.3	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)c(C)n1C	10.1016/j.bmcl.2004.05.003
		71458058	85822	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	625	8	3	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CCC2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113152	85822	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	625	8	3	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CCC2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		11477853	73668	0	None	-38	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
		CHEMBL186439	73668	0	None	-38	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
		44562365	182914	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	575	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL459217	182914	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	575	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44393421	129881	0	None	4	4	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	508	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL361052	129881	0	None	4	4	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	508	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44444465	101006	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	7	2	5	5.3	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3ccccc3N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249986	101006	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	7	2	5	5.3	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3ccccc3N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415537	146451	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccccc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL379792	146451	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccccc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		44265715	16957	0	None	-4	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL1159702	16957	0	None	-4	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		44434661	95288	0	None	-3	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	415	11	2	3	4.4	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL235136	95288	0	None	-3	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	415	11	2	3	4.4	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1	10.1016/j.bmc.2007.06.003
		44434761	95942	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	625	11	3	3	8.9	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236626	95942	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	625	11	3	3	8.9	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434647	96365	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.3	NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3	10.1016/j.bmc.2007.06.003
		CHEMBL237483	96365	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.3	NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3	10.1016/j.bmc.2007.06.003
		44434605	156293	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	356	10	1	3	4.4	C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1	10.1016/j.bmc.2007.06.003
		CHEMBL394647	156293	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	356	10	1	3	4.4	C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1	10.1016/j.bmc.2007.06.003
		137660671	165997	0	None	-147	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4098785	165997	0	None	-147	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		137636677	162879	0	None	-28	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4063111	162879	0	None	-28	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		168272746	197303	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5179536	197303	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL3644287	218710	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644287	218710	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644281	218704	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644281	218704	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		88590642	131845	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		CHEMBL3644360	131845	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		88590642	131845	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		CHEMBL3644360	131845	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		44393823	130752	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL362880	130752	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		2726	7706	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	7706	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	7706	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	7706	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	7706	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		44412511	84715	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC)C(=O)C(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209558	84715	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC)C(=O)C(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL438596	220560	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		11180881	73595	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2005.03.053
		CHEMBL186074	73595	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2005.03.053
		44562399	183742	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	10	2	5	4.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462346	183742	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	10	2	5	4.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		11180881	73595	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186074	73595	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2004.08.055
		88590610	131838	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644306	131838	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644315	218734	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O	nan
		CHEMBL3644349	218767	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3646872	218790	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590610	131838	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644306	131838	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644315	218734	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O	nan
		CHEMBL3644349	218767	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3646872	218790	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88287712	134339	0	None	36	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1154	19	17	12	-1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3663364	134339	0	None	36	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1154	19	17	12	-1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3663373	218881	0	None	9	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL2415081	217211	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		CHEMBL2415083	217213	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		168281969	198057	0	None	2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190661	198057	0	None	2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433442	96960	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	5	1	5	5.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL238197	96960	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	5	1	5	5.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44412911	175773	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	12	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL439168	175773	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	12	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL5080489	221468	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44322787	112741	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL312998	112741	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		24886499	18593	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182090	18593	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211202	18593	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44562596	181235	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	545	10	1	5	5.1	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL455394	181235	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	545	10	1	5	5.1	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		44322987	103507	0	None	-4	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL264306	103507	0	None	-4	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44396158	73943	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	10	4	6	3.0	CC(N[C@@H]1CCCC[C@H]1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL187690	73943	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	10	4	6	3.0	CC(N[C@@H]1CCCC[C@H]1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415018	217208	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44405558	78565	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	12	2	4	4.8	CCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL196758	78565	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	12	2	4	4.8	CCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44404566	77326	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1cccc(C(F)(F)F)c1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL194761	77326	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1cccc(C(F)(F)F)c1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404575	79296	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1c(F)cccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199071	79296	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1c(F)cccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71454508	85818	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	3	5	3.5	CNC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113148	85818	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	3	5	3.5	CNC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		71450912	85747	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	588	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2113033	85747	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	588	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11341046	73654	0	None	-57	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	7	4	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1	10.1021/jm0400496
		CHEMBL186339	73654	0	None	-57	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	7	4	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1	10.1021/jm0400496
		44392535	71046	0	None	-2	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	8	2	7	2.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL180937	71046	0	None	-2	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	8	2	7	2.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44415765	87913	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	7	1	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc3c(c2)OCO3)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215697	87913	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	7	1	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc3c(c2)OCO3)CC1	10.1016/j.bmcl.2006.05.088
		44412677	145446	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.1	COc1ccc(C(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL377761	145446	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.1	COc1ccc(C(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		44412931	147773	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	12	5	8	0.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(CO)CO)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL382353	147773	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	12	5	8	0.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(CO)CO)CC1	10.1016/j.bmcl.2006.04.069
		44416025	86742	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	533	7	1	4	6.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CSc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212664	86742	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	533	7	1	4	6.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CSc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434696	155977	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	11	3	3	8.4	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL394394	155977	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	11	3	3	8.4	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434762	159789	0	None	1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397550	159789	0	None	1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44443044	100664	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	8	0	5	5.1	CC(=O)N(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248057	100664	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	8	0	5	5.1	CC(=O)N(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347987	171117	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	5	1	2	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.05.003
		CHEMBL421254	171117	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	5	1	2	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.05.003
		44265707	16956	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	354	10	3	4	2.1	C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL1159701	16956	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	354	10	3	4	2.1	C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		71454518	85925	0	None	-10	4	Human	4.8	pKi	=	4.8	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	456	10	4	3	3.3	NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL2113315	85925	0	None	-10	4	Human	4.8	pKi	=	4.8	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	456	10	4	3	3.3	NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		9842665	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44404543	79151	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	4	1.4	CCN(CC(c1ccccc1F)N1CCN(C)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.08.018
		CHEMBL198607	79151	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	4	1.4	CCN(CC(c1ccccc1F)N1CCN(C)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.08.018
		44413879	145680	0	None	-123	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL378293	145680	0	None	-123	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL5081077	221496	0	None	-32	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137647538	164741	0	None	-275	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4084765	164741	0	None	-275	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44400708	75456	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	12	2	7	5.9	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1nccs1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192153	75456	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	12	2	7	5.9	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1nccs1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562457	196112	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL512496	196112	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		122178157	128030	0	None	50	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577986	128030	0	None	50	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178164	128036	0	None	158	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577993	128036	0	None	158	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		11636019	79135	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198535	79135	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44405426	142564	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL373037	142564	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416201	148406	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL385274	148406	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44447785	101852	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255313	101852	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443032	100934	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	1	6	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(OC)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL249473	100934	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	1	6	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(OC)c1	10.1016/j.bmcl.2007.10.032
		9842665	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmcl.2005.03.053
		CHEMBL40711	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmcl.2005.03.053
		44322958	113789	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL315356	113789	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44323033	113929	0	None	-5	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL316259	113929	0	None	-5	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44322788	164162	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL407825	164162	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391272	138573	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	670	12	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL369348	138573	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	670	12	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		10033237	75846	0	None	-933	3	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		CHEMBL1923662	75846	0	None	-933	3	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		CHEMBL3577977	218524	0	None	3	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577979	218526	0	None	8	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577982	218529	0	None	3	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577988	218530	0	None	-	1	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433422	95498	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	562	6	1	4	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236109	95498	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	562	6	1	4	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415453	87002	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CCC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213739	87002	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CCC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405553	164922	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	2	4	4.0	CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL408721	164922	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	2	4	4.0	CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44416163	148563	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	457	8	1	4	4.9	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(Cl)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL386162	148563	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	457	8	1	4	4.9	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(Cl)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		9842665	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		70681743	81855	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	542	10	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		CHEMBL2035942	81855	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	542	10	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		44447774	161993	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	468	5	1	4	4.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL402588	161993	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	468	5	1	4	4.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44444462	100978	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	517	7	1	5	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3cccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249780	100978	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	517	7	1	5	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3cccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415766	145510	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	2	3	5.8	Cc1[nH]c2ccccc2c1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL378016	145510	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	2	3	5.8	Cc1[nH]c2ccccc2c1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		44416228	86780	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212802	86780	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434766	161493	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL399810	161493	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44348035	120565	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	412	6	0	3	5.8	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C(C)C)cn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL332382	120565	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	412	6	0	3	5.8	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C(C)C)cn1C	10.1016/j.bmcl.2004.05.003
		71456250	85802	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	557	6	3	5	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113132	85802	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	557	6	3	5	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		23653113	95427	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	9	4	2	4.2	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235798	95427	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	9	4	2	4.2	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10293285	96387	0	None	-2	3	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	382	7	1	2	4.9	NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL237528	96387	0	None	-2	3	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	382	7	1	2	4.9	NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		10137615	96511	0	None	-6	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	9	2	2	5.4	CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237692	96511	0	None	-6	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	9	2	2	5.4	CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10108894	96512	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	355	8	2	2	4.4	NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1	10.1016/j.bmc.2007.06.003
		CHEMBL237693	96512	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	355	8	2	2	4.4	NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1	10.1016/j.bmc.2007.06.003
		44434652	96676	0	None	-7	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	403	12	2	2	5.2	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237912	96676	0	None	-7	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	403	12	2	2	5.2	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434614	158363	1	None	1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.9	NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396341	158363	1	None	1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.9	NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434857	161206	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	475	13	2	4	3.9	NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL398980	161206	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	475	13	2	4	3.9	NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		88944293	160494	0	None	-6606	2	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	15	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3981581	160494	0	None	-6606	2	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	15	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		168295726	199184	0	None	-263	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5207936	199184	0	None	-263	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL3644339	218758	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644339	218758	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168276294	197287	0	None	-79	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	3264	55	36	40	1.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5179373	197287	0	None	-79	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	3264	55	36	40	1.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44447780	101819	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255100	101819	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442995	100427	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL246837	100427	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44413914	146296	0	None	-26	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL379508	146296	0	None	-26	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44444505	101283	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL251594	101283	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44410802	147163	0	None	114	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	1	5	5.3	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380858	147163	0	None	114	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	1	5	5.3	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1	10.1016/j.bmcl.2005.10.103
		44432955	93982	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232773	93982	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44322957	212990	0	None	-2	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL86573	212990	0	None	-2	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88185	222675	0	None	1	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11753668	127147	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL353239	127147	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405443	79356	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	568	11	2	5	3.2	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199273	79356	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	568	11	2	5	3.2	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44413005	86664	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	3	6	2.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCC(F)(F)F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212358	86664	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	3	6	2.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCC(F)(F)F)CC1	10.1016/j.bmcl.2006.04.069
		44447222	101393	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	10	1	6	5.1	CC(C)C[C@H](NCCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252234	101393	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	10	1	6	5.1	CC(C)C[C@H](NCCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415434	145263	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL377480	145263	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447210	161661	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	624	10	2	5	6.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400738	161661	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	624	10	2	5	6.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		71454509	85820	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	627	9	2	5	4.6	CCN(CC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113150	85820	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	627	9	2	5	4.6	CCN(CC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44323212	175498	0	None	-1	2	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		CHEMBL436903	175498	0	None	-1	2	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		44562283	195695	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	573	14	0	4	7.4	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL507776	195695	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	573	14	0	4	7.4	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		11272336	63968	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164969	63968	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		11364343	126702	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349427	126702	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44444431	101146	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	7	1	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNS(C)(=O)=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250778	101146	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	7	1	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNS(C)(=O)=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415370	175719	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL438793	175719	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44416214	86798	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212882	86798	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44434689	95950	0	None	-14	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	14	2	2	5.9	NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236649	95950	0	None	-14	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	14	2	2	5.9	NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434635	175666	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	363	10	2	2	4.3	NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL438334	175666	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	363	10	2	2	4.3	NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44432891	94576	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233809	94576	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL3644335	218754	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134145039	157388	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	18	17	12	2.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCN)/N=C\1O	nan
		CHEMBL3955264	157388	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	18	17	12	2.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCN)/N=C\1O	nan
		44413969	87005	0	None	-5	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL213752	87005	0	None	-5	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL3644281	218704	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644281	218704	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		46885526	14536	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL1089135	14536	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL1204056	14536	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL438596	220560	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		46885761	14800	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
		CHEMBL1090813	14800	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
		10304794	146183	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	146183	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44432891	94576	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233809	94576	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44400707	75088	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	570	12	2	5	5.6	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCC1CC1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191645	75088	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	570	12	2	5	5.6	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCC1CC1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400658	75413	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	559	12	3	6	4.2	NCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191831	75413	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	559	12	3	6	4.2	NCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562288	181029	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454901	181029	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		24180592	103788	0	None	-5	6	Mouse	7.8	pKi	=	7.8	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL266647	103788	0	None	-5	6	Mouse	7.8	pKi	=	7.8	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL3663360	218869	0	None	91	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL2415019	217209	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCCc1cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44433444	96961	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	7	1	5	5.2	CCN1CCC(N2C[C@@H](C(=O)N3CCN(c4ccc(C)cc4[C@@H](N)C(C)C)CC3)[C@H](c3ccc(Cl)cc3)C2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL238198	96961	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	7	1	5	5.2	CCN1CCC(N2C[C@@H](C(=O)N3CCN(c4ccc(C)cc4[C@@H](N)C(C)C)CC3)[C@H](c3ccc(Cl)cc3)C2)CC1	10.1016/j.bmcl.2007.09.079
		44433445	175753	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	1	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(C(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL439040	175753	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	1	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(C(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44415693	86623	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CCC(C)[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212192	86623	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CCC(C)[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444510	161911	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL402060	161911	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL267492	217503	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432955	93982	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232773	93982	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447780	101819	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255100	101819	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447803	101840	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	546	6	1	5	5.3	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255261	101840	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	546	6	1	5	5.3	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44413931	84790	0	None	1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL209789	84790	0	None	1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44397029	73879	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	661	13	3	7	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1OC	10.1016/j.bmcl.2005.05.017
		CHEMBL187390	73879	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	661	13	3	7	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1OC	10.1016/j.bmcl.2005.05.017
		44397282	130199	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	573	11	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361693	130199	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	573	11	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412613	145704	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378411	145704	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		44412646	146047	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	552	11	2	4	5.4	CC(C)CC(CC(C)C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379051	146047	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	552	11	2	4	5.4	CC(C)CC(CC(C)C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		10304794	146183	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	146183	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL89270	222678	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1016/s0960-894x(03)00552-3
		44433386	95306	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	8	2	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(CCN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235215	95306	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	8	2	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(CCN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44412912	86653	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	521	10	2	6	2.9	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212308	86653	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	521	10	2	6	2.9	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		44447225	101696	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	2	6	4.3	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254279	101696	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	2	6	4.3	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44405374	142051	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3ccccc3F)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL372621	142051	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3ccccc3F)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447230	161668	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.5	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400787	161668	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.5	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44577056	194537	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	413	6	1	3	4.5	CC(C)[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL495674	194537	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	413	6	1	3	4.5	CC(C)[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44447816	102184	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256955	102184	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443003	160640	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	590	8	1	4	5.7	O=C(C1CCCC1)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398285	160640	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	590	8	1	4	5.7	O=C(C1CCCC1)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25132524	183537	0	None	5	3	Human	6.8	pKi	=	6.8	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		CHEMBL460349	183537	0	None	5	3	Human	6.8	pKi	=	6.8	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		9977350	23066	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1ncc(C)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL122491	23066	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1ncc(C)n1C	10.1016/j.bmcl.2004.05.003
		44347980	23210	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	430	5	0	3	5.7	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL123263	23210	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	430	5	0	3	5.7	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		71459942	85821	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	655	11	2	5	5.4	CCCN(CCC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113151	85821	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	655	11	2	5	5.4	CCCN(CCC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397079	134330	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	539	11	3	5	3.5	CC(C)CNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL366313	134330	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	539	11	3	5	3.5	CC(C)CNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44395646	73822	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	468	8	2	5	4.1	NC(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL187147	73822	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	468	8	2	5	4.1	NC(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44415631	86714	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	1	4	5.9	CCC(C)[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212553	86714	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	1	4	5.9	CCC(C)[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44412684	145705	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	628	11	3	8	3.4	COc1ccccc1OC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378412	145705	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	628	11	3	8	3.4	COc1ccccc1OC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44412740	146056	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	3	7	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379091	146056	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	3	7	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44412676	176082	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	582	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL441532	176082	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	582	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		70681741	81852	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	492	10	2	4	2.8	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(F)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035939	81852	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	492	10	2	4	2.8	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(F)c1	10.1016/j.bmc.2012.04.001
		44447811	161813	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	462	5	1	4	3.7	CC(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401585	161813	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	462	5	1	4	3.7	CC(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443038	161670	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	622	11	0	5	6.8	COc1ccc(CN(CC(C)C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL400789	161670	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	622	11	0	5	6.8	COc1ccc(CN(CC(C)C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44434865	95525	0	None	-5	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	589	10	4	3	6.5	NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL236226	95525	0	None	-5	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	589	10	4	3	6.5	NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44434632	153087	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	10	2	2	4.4	NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL392096	153087	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	10	2	2	4.4	NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		9842665	163585	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		88213487	149694	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1088	20	18	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3893834	149694	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1088	20	18	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644340	218759	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)CNC(N)=O)NC1=O	nan
		44401573	77973	0	None	-1	2	Human	5.7	pKi	=	5.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	568	13	5	4	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL195638	77973	0	None	-1	2	Human	5.7	pKi	=	5.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	568	13	5	4	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		89703080	158689	0	None	-61	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	970	17	12	10	-0.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	nan
		CHEMBL3966157	158689	0	None	-61	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	970	17	12	10	-0.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	nan
		44413830	84725	0	None	-1	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL209622	84725	0	None	-1	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44415991	87285	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL214770	87285	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
		44415991	87285	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
		CHEMBL214770	87285	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
		CHEMBL3644287	218710	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644300	218722	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646850	218774	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3646854	218777	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		134153231	159341	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		CHEMBL3971748	159341	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		CHEMBL3644287	218710	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644300	218722	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646850	218774	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		1324	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		16154396	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		16197727	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		44285019	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		57514683	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		91898441	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		CHEMBL441738	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		DB04931	7090	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		44393885	131165	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363925	131165	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
		16007264	86495	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL211564	86495	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		16007264	86495	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL211564	86495	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		25132526	195702	0	None	43	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
		CHEMBL507876	195702	0	None	43	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
		10408	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		5329	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		9941379	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		CHEMBL2070241	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		DB11653	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		168281421	197736	0	None	-346	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5185945	197736	0	None	-346	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432959	94022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232972	94022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		46877881	208597	0	None	2	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL606990	208597	0	None	2	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		9983075	84083	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL208268	84083	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
		44415522	88235	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	8	1	3	6.5	CCCCC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215974	88235	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	8	1	3	6.5	CCCCC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444460	100949	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	1	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CC3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249575	100949	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	1	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CC3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447223	101394	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	10	2	6	4.6	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252235	101394	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	10	2	6	4.6	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447769	102387	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257828	102387	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44447805	162155	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL403431	162155	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44442999	101231	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	7	1	4	4.5	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251287	101231	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	7	1	4	4.5	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443001	101232	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	9	1	4	5.3	CCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251288	101232	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	9	1	4	5.3	CCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443037	161669	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	0	5	6.1	CCN(Cc1ccc(OC)cc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL400788	161669	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	0	5	6.1	CCN(Cc1ccc(OC)cc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44404546	78909	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197859	78909	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404572	140345	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	305	7	0	4	2.3	CCN(CC)CC(c1ccccc1OC)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL371105	140345	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	305	7	0	4	2.3	CCN(CC)CC(c1ccccc1OC)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		58777970	85811	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113141	85811	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397308	74301	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	605	10	3	5	3.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189601	74301	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	605	10	3	5	3.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11179914	126960	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL351705	126960	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		46930943	75180	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2011.08.053
		CHEMBL1917059	75180	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2011.08.053
		44415709	87918	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	8	1	3	6.6	CN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215712	87918	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	8	1	3	6.6	CN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434707	156326	0	None	1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL394667	156326	0	None	1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44434763	158122	0	None	-3	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	685	13	3	5	9.0	COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL396111	158122	0	None	-3	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	685	13	3	5	9.0	COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434765	168550	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	643	11	3	3	9.1	NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL413982	168550	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	643	11	3	3	9.1	NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434592	96290	0	None	-5	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237315	96290	0	None	-5	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		168269216	196656	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169353	196656	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44320339	212902	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	410	9	1	2	6.0	NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL85918	212902	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	410	9	1	2	6.0	NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		44433293	151701	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391028	151701	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400934	77388	0	None	173	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	10	2	5	4.9	CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194987	77388	0	None	173	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	10	2	5	4.9	CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400662	131946	0	None	478	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	13	3	6	4.5	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL364463	131946	0	None	478	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	13	3	6	4.5	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562475	192792	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	519	9	3	5	3.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487043	192792	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	519	9	3	5	3.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562402	195542	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	644	12	1	6	6.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL505442	195542	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	644	12	1	6	6.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644321	218740	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3646857	218780	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646858	218781	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590671	132307	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646870	132307	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590671	132307	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646870	132307	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134134523	150565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3901055	150565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3646857	218780	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646858	218781	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88287608	134336	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1066	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663333	134336	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1066	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663326	218837	0	None	-1	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663353	218862	0	None	213	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663356	218865	0	None	436	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667915	218891	0	None	16	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3667938	218911	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667942	218915	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944366	154800	0	None	-19	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3934498	154800	0	None	-19	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44349471	23645	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL124954	23645	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		44456184	162267	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL404069	162267	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		10077773	94042	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233135	94042	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44412612	145703	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	145703	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		44432949	93565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232161	93565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44400809	75177	0	None	407	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	599	11	3	5	5.1	O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191701	75177	0	None	407	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	599	11	3	5	5.1	O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44456137	161900	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
		CHEMBL402017	161900	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
		44432949	93565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232161	93565	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44443030	100901	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	1	5	6.2	CC(C)Oc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL249271	100901	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	1	5	6.2	CC(C)Oc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432943	157009	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395226	157009	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL2370533	216647	0	None	9	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		44456183	104798	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272956	104798	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		23635108	151741	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635108	151741	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL391056	151741	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL391056	151741	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL267492	217503	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432943	157009	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395226	157009	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL385556	219133	0	None	29	3	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44434563	95474	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236015	95474	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44433285	95391	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235640	95391	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400811	75416	0	None	416	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	615	10	3	5	5.7	CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191857	75416	0	None	416	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	615	10	3	5	5.7	CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400660	77505	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195071	77505	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415080	217210	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		44400660	77505	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL195071	77505	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL439128	220604	0	None	2	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44434555	96179	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237050	96179	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		24740419	154973	0	None	478	4	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL393584	154973	0	None	478	4	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL412494	219776	0	None	19	3	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44433297	159825	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397582	159825	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44432931	94528	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233757	94528	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432931	94528	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233757	94528	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44400777	75447	0	None	295	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	630	13	2	7	4.7	COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192090	75447	0	None	295	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	630	13	2	7	4.7	COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410176	82799	7	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
		CHEMBL205594	82799	7	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
		23635107	98333	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635107	98333	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240571	98333	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240571	98333	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		23635235	173280	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635235	173280	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL427860	173280	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL427860	173280	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		6918850	132200	1	None	154	4	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL364560	132200	1	None	154	4	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44400813	77861	0	None	120	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	603	12	4	6	3.9	O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195308	77861	0	None	120	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	603	12	4	6	3.9	O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44432963	94227	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233371	94227	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432963	94227	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233371	94227	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL266417	217462	0	None	8	3	Human	7.7	pKi	=	7.7	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		CHEMBL3646877	218795	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646877	218795	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88287431	135429	0	None	13	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667923	135429	0	None	13	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3639622	218697	0	None	1	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		88944369	157589	0	None	-1412	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	21	16	11	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3956787	157589	0	None	-1412	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	21	16	11	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3577981	218528	1	None	29	3	Mouse	7.7	pKi	=	7.7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44416298	148670	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	459	7	1	3	5.4	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL386771	148670	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	459	7	1	3	5.4	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		1338	10579	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44432959	94022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232972	94022	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44404571	79092	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)CC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198379	79092	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)CC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		6918857	145487	1	None	33	4	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377961	145487	1	None	33	4	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		9915636	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL186083	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44433425	95553	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	556	10	1	6	4.3	COCC(COC)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL236319	95553	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	556	10	1	6	4.3	COCC(COC)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447232	101537	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.9	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL253205	101537	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.9	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412930	145167	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	13	3	7	2.6	CCC(COC)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377258	145167	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	13	3	7	2.6	CCC(COC)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44416209	145718	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.4	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1F	10.1016/j.bmcl.2006.06.075
		CHEMBL378448	145718	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.4	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1F	10.1016/j.bmcl.2006.06.075
		44443008	104901	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	585	9	1	5	5.6	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL273565	104901	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	585	9	1	5	5.6	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44404567	79270	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199003	79270	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44416073	146080	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL379200	146080	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2006.06.075
		44434690	96081	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	96081	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434766	161493	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL399810	161493	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44347766	121322	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	7	0	3	6.2	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1CC1CC1	10.1016/j.bmcl.2004.05.003
		CHEMBL333702	121322	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	7	0	3	6.2	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1CC1CC1	10.1016/j.bmcl.2004.05.003
		763557	131109	42	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	190	2	0	2	1.4	CN1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL363603	131109	42	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	190	2	0	2	1.4	CN1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2005.08.018
		44265374	213267	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	454	10	2	2	6.4	O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL8825	213267	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	454	10	2	2	6.4	O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168269216	196656	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169353	196656	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168270860	196687	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169826	196687	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5077811	221295	0	None	-36	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
		CHEMBL3644283	218706	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644283	218706	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		88944287	158926	0	None	-5128	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	972	16	13	10	-0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)Cc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3968105	158926	0	None	-5128	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	972	16	13	10	-0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)Cc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		44433455	154223	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	7	1	4	5.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCC(F)(F)F)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL393010	154223	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	7	1	4	5.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCC(F)(F)F)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44455923	161981	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)ccc2F)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL402510	161981	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)ccc2F)CC1	10.1016/j.bmcl.2007.10.115
		9915636	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL186083	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410041	148043	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
		CHEMBL383120	148043	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
		44562398	183741	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	550	12	2	5	5.6	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462345	183741	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	550	12	2	5	5.6	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44562459	185799	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	562	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471167	185799	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	562	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		9915636	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186083	73598	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44433448	95259	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234983	95259	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433448	95259	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL234983	95259	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44412869	146918	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	559	10	2	6	4.2	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL380222	146918	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	559	10	2	6	4.2	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		16132144	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		16133793	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		44273719	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		CHEMBL214332	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		44413930	145426	0	None	1	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377620	145426	0	None	1	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44397199	130411	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	619	11	3	5	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361882	130411	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	619	11	3	5	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		10408	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		5329	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		9941379	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		CHEMBL2070241	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		DB11653	7507	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		44323015	118210	0	None	-3	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL327450	118210	0	None	-3	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44396141	73030	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	568	12	3	6	3.2	CC(NCCN1CCCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184623	73030	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	568	12	3	6	3.2	CC(NCCN1CCCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		11456260	163275	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL406764	163275	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405365	78721	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197278	78721	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44405596	78783	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	11	2	4	4.4	CCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197446	78783	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	11	2	4	4.4	CCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44415398	87051	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	2	5	5.1	NCCC(=O)NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213953	87051	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	2	5	5.1	NCCC(=O)NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44577055	200075	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL524060	200075	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44443002	101262	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.2	CC(C)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251494	101262	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.2	CC(C)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443000	175669	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	550	8	1	4	4.9	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL438348	175669	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	550	8	1	4	4.9	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44397222	74215	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	620	10	4	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189032	74215	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	620	10	4	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397129	131039	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	621	10	3	5	4.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL363445	131039	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	621	10	3	5	4.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44447247	101476	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252824	101476	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415545	148187	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	3	5.3	Cc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL384040	148187	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	3	5.3	Cc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416046	87862	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	473	6	1	5	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cn2cnc3ccccc32)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215531	87862	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	473	6	1	5	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cn2cnc3ccccc32)CC1	10.1016/j.bmcl.2006.06.075
		44434694	95376	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	665	14	3	5	8.7	CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL235589	95376	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	665	14	3	5	8.7	CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		44434706	96372	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237504	96372	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44434855	96805	0	None	-2	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	96805	0	None	-2	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434870	154927	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL393553	154927	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44434693	174126	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	559	12	2	4	7.4	CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL429451	174126	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	559	12	2	4	7.4	CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		9842665	163585	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		71461656	85804	7	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	543	6	3	5	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113134	85804	7	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	543	6	3	5	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44265496	103824	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL267020	103824	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		44434613	96364	0	None	1	2	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	8	2	3	5.1	NCCCN(C(=O)c1cc2cc(OCc3ccccc3)ccc2[nH]1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237479	96364	0	None	1	2	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	8	2	3	5.1	NCCCN(C(=O)c1cc2cc(OCc3ccccc3)ccc2[nH]1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		44434658	97010	0	None	-2	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL238342	97010	0	None	-2	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		44434580	158682	0	None	1	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	335	8	2	2	3.5	NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396598	158682	0	None	1	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	335	8	2	2	3.5	NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		11851038	147113	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		168296647	199254	0	None	-33	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5208830	199254	0	None	-33	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44409379	83297	0	None	57	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL206018	83297	0	None	57	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		44409337	177240	0	None	39	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL444883	177240	0	None	39	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		89008025	160293	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1069	18	16	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3979831	160293	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1069	18	16	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644308	218727	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44413600	19070	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184893	19070	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL376936	19070	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44432899	93802	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232533	93802	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL410168	219583	0	None	3	3	Human	7.7	pKi	=	7.7	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44391304	137231	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	692	13	2	6	5.0	CN(C)CCN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL368022	137231	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	692	13	2	6	5.0	CN(C)CCN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644279	218702	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644279	218702	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		16132144	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44442943	161460	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399667	161460	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44397125	73838	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	657	12	3	6	4.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187224	73838	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	657	12	3	6	4.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168293710	198945	0	None	-91	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5203986	198945	0	None	-91	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44322868	112785	0	None	-37	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313279	112785	0	None	-37	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44409140	148064	0	None	10	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL383256	148064	0	None	10	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		44395948	130203	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.8	CN(CCc1cccs1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL361714	130203	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.8	CN(CCc1cccs1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		9960253	123727	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL338594	123727	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44433413	95352	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	5	1	4	4.0	CC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235460	95352	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	5	1	4	4.0	CC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44444432	101179	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250976	101179	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44432899	93802	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232533	93802	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		44442954	101074	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL250495	101074	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44442972	159797	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397562	159797	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		9960253	123727	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.07.035
		CHEMBL338594	123727	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.07.035
		44397279	73909	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3CCCCC3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187521	73909	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3CCCCC3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397196	130846	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	590	10	4	6	2.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C3=CNCC=C3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL363239	130846	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	590	10	4	6	2.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C3=CNCC=C3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397307	172769	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	10	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL425353	172769	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	10	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2415017	217207	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmc.2013.06.052
		44412711	84947	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL210450	84947	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		44415546	87013	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccc(C(F)(F)F)c2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213776	87013	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccc(C(F)(F)F)c2)CC1	10.1016/j.bmcl.2006.05.088
		44416007	87855	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	505	9	1	4	5.7	CCOc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL215502	87855	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	505	9	1	4	5.7	CCOc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		44434697	155472	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	543	10	2	4	6.8	COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL393994	155472	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	543	10	2	4	6.8	COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44443009	101298	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.7	O=C([C@H]1CNC[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL251699	101298	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.7	O=C([C@H]1CNC[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		168270860	196687	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169826	196687	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44415972	86658	0	None	5	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
		CHEMBL212332	86658	0	None	5	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
		44413832	84840	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL210009	84840	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		44401607	140395	0	None	2	2	Human	6.7	pKi	=	6.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	635	15	6	4	3.7	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL371366	140395	0	None	2	2	Human	6.7	pKi	=	6.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	635	15	6	4	3.7	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44432920	94527	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233756	94527	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		44433288	168046	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	11	1	5	4.8	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL412024	168046	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	11	1	5	4.8	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400612	76161	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	2	5	5.9	CC(C)CN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL193061	76161	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	2	5	5.9	CC(C)CN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400768	132848	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	650	12	2	6	6.6	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL364913	132848	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	650	12	2	6	6.6	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44562541	178910	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	612	12	3	6	4.4	COc1ccc(CCC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2008.07.076
		CHEMBL447298	178910	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	612	12	3	6	4.4	COc1ccc(CCC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2008.07.076
		88590600	131834	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		CHEMBL3644294	131834	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		88590591	131837	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644305	131837	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644312	218731	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88590600	131834	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		CHEMBL3644294	131834	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		88590591	131837	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644305	131837	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644312	218731	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44393886	73133	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185145	73133	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44577089	185526	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL468579	185526	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		9867330	104617	0	None	100	2	Human	7.6	pKi	=	7.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
		CHEMBL272099	104617	0	None	100	2	Human	7.6	pKi	=	7.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
		44397027	74213	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	635	11	3	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189004	74213	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	635	11	3	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44562595	195667	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	549	12	1	5	5.8	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL507347	195667	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	549	12	1	5	5.8	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		11490215	63928	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164671	63928	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405562	79208	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	592	10	2	4	4.8	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198785	79208	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	592	10	2	4	4.8	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44444450	100881	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	483	8	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNCCN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249168	100881	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	483	8	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNCCN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447218	161597	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	654	10	1	5	5.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400379	161597	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	654	10	1	5	5.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416227	146021	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		CHEMBL378913	146021	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		71452735	85823	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CO2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113153	85823	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CO2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44397195	74262	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	593	10	3	6	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189341	74262	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	593	10	3	6	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44400824	76614	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	621	12	3	6	5.7	O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL193786	76614	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	621	12	3	6	5.7	O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44415726	84805	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	503	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2csc3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209869	84805	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	503	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2csc3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44434764	95335	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	551	10	2	2	7.8	NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235358	95335	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	551	10	2	2	7.8	NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434653	152593	0	None	-2	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	12	2	2	5.7	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391706	152593	0	None	-2	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	12	2	2	5.7	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434703	152886	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL391944	152886	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434762	159789	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397550	159789	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44432920	94527	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233756	94527	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		44434599	96694	0	None	-1	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	333	7	2	2	3.7	NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237957	96694	0	None	-1	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	333	7	2	2	3.7	NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		16132144	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		46885368	14728	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
		CHEMBL1090484	14728	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
		168279557	197640	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5184591	197640	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		11845444	86842	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL213026	86842	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168279557	197640	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5184591	197640	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44409257	147364	0	None	67	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		CHEMBL381357	147364	0	None	67	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		44562414	183596	0	None	13	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL460942	183596	0	None	13	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44391380	130722	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.6	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)Cc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL362850	130722	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.6	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)Cc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		11421919	126759	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL349887	126759	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL3646855	218778	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		134153811	159348	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		CHEMBL3971788	159348	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		44393862	130459	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL362147	130459	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44393822	130821	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363074	130821	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44577064	194696	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL496710	194696	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44447777	162194	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403675	162194	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443019	161534	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccc(F)c4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400058	161534	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccc(F)c4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10408	7507	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		5329	7507	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		9941379	7507	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		CHEMBL2070241	7507	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		DB11653	7507	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		44433282	95458	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	634	13	2	5	5.6	CC(C)C[C@H](NCCCC(=O)O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235955	95458	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	634	13	2	5	5.6	CC(C)C[C@H](NCCCC(=O)O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		71458046	85739	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	2	6	3.2	CN1CCN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113022	85739	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	2	6	3.2	CN1CCN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		44444457	100922	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	7	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249378	100922	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	7	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416208	145707	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1C	10.1016/j.bmcl.2006.06.075
		CHEMBL378425	145707	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1C	10.1016/j.bmcl.2006.06.075
		71458057	85815	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	3	5	3.2	NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113145	85815	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	3	5	3.2	NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397130	133319	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	665	10	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Br)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365223	133319	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	665	10	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Br)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11261324	64908	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL167780	64908	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44415660	87048	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	4	6.7	CCC(C)[C@H](NC(=O)OC)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213935	87048	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	4	6.7	CCC(C)[C@H](NC(=O)OC)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434692	95300	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	651	13	3	5	8.3	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL235176	95300	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	651	13	3	5	8.3	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434587	96213	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	6	2	3	3.9	NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237094	96213	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	6	2	3	3.9	NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		44434767	96510	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	616	11	3	4	8.2	N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237689	96510	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	616	11	3	4	8.2	N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44265315	212711	0	None	-2	2	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	485	15	5	4	4.6	NCCCCNC(=O)[C@H](CCCCNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8418	212711	0	None	-2	2	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	485	15	5	4	4.6	NCCCCNC(=O)[C@H](CCCCNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44401592	131968	0	None	4	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	607	13	6	4	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL364519	131968	0	None	4	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	607	13	6	4	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44413536	146707	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379959	146707	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		168279751	197967	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	66	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5189180	197967	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	66	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168286511	198124	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	70	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5191823	198124	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	70	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL50056	220898	2	None	-7	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm060384p
		11846844	146857	0	None	-1	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL380051	146857	0	None	-1	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL3646860	218783	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646860	218783	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		44393863	134331	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL366321	134331	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44415479	87880	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215601	87880	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		16046215	86864	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL213122	86864	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		16132144	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16046215	86864	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
		CHEMBL213122	86864	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
		44443015	100821	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248862	100821	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL5077095	221258	0	None	-22	3	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL5090946	222064	0	None	-18	3	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL2415086	217216	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		70693083	83704	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929813	83704	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070253	83704	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44433419	95444	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	6	1	4	4.7	CC(C)C(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235892	95444	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	6	1	4	4.7	CC(C)C(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44456461	164765	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	619	10	1	5	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)c(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL408511	164765	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	619	10	1	5	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)c(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44397131	73559	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL185934	73559	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44444434	101251	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1cncn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL251380	101251	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1cncn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447212	101378	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	9	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252180	101378	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	9	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44397131	73559	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL185934	73559	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		10031074	83118	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
		CHEMBL205898	83118	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
		44415360	84754	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	541	9	1	5	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)c(OC)c2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209682	84754	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	541	9	1	5	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)c(OC)c2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415791	87179	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(OC)c(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL214537	87179	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(OC)c(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416044	87186	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214559	87186	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44416043	87193	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214582	87193	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434753	96509	0	None	1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	699	12	3	4	9.1	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		CHEMBL237688	96509	0	None	1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	699	12	3	4	9.1	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		44434862	97023	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238368	97023	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44348033	22859	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	446	7	0	3	6.7	CCC(C)n1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL122382	22859	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	446	7	0	3	6.7	CCC(C)n1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		71452732	85809	0	None	-3	4	Human	5.6	pKi	=	5.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	697	8	2	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113139	85809	0	None	-3	4	Human	5.6	pKi	=	5.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	697	8	2	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		10225762	152595	0	None	-3	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	448	14	2	3	5.5	CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL391707	152595	0	None	-3	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	448	14	2	3	5.5	CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434858	174030	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL429269	174030	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		10025669	104167	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL269776	104167	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1021/jm020945m
		137655905	165607	0	None	-69	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4094606	165607	0	None	-69	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		56851057	75847	0	None	-1071	3	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1069	34	13	10	1.3	C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1021/jm201226w
		CHEMBL1923664	75847	0	None	-1071	3	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1069	34	13	10	1.3	C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1021/jm201226w
		44401285	142453	0	None	3	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	636	13	5	4	4.1	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL372966	142453	0	None	3	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	636	13	5	4	4.1	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		16132144	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		168291110	198799	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5201799	198799	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433263	95968	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236732	95968	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416361	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL386259	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44433291	159570	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397367	159570	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416361	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL386259	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44410046	82726	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
		CHEMBL205214	82726	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
		44562599	181041	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.3	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454918	181041	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.3	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562423	196363	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	9	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL514603	196363	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	9	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		44562497	200976	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	10	3	5	3.6	CCCC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL528329	200976	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	10	3	5	3.6	CCCC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44395950	130826	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCNCC1	10.1016/j.bmcl.2004.08.055
		CHEMBL363122	130826	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCNCC1	10.1016/j.bmcl.2004.08.055
		49857745	131842	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644354	131842	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		49857745	131842	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644354	131842	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		16132144	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		16133793	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		44273719	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		CHEMBL214332	216058	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		44434551	95943	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(F)cc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236627	95943	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(F)cc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44433263	95968	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236732	95968	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433562	95490	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	515	6	1	3	6.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236063	95490	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	515	6	1	3	6.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44433480	95865	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236527	95865	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433384	161489	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL399801	161489	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433384	161489	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL399801	161489	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44577087	185248	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	4	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL466346	185248	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	4	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		44416361	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL386259	148583	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44442931	157169	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL395355	157169	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133207	179722	0	None	16	3	Human	7.6	pKi	=	7.6	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
		CHEMBL451694	179722	0	None	16	3	Human	7.6	pKi	=	7.6	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
		44412512	84716	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	629	11	3	6	3.4	CS(=O)(=O)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209559	84716	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	629	11	3	6	3.4	CS(=O)(=O)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		10257541	133120	0	None	123	4	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL365039	133120	0	None	123	4	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44433418	95400	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	7	1	4	4.8	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235676	95400	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	7	1	4	4.8	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44455892	104695	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL272515	104695	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		44433387	158740	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	598	7	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL396657	158740	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	598	7	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405375	147130	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
		CHEMBL380769	147130	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
		44447228	161392	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	6	1	5	5.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399241	161392	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	6	1	5	5.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		11851038	147113	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		24740311	96026	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236802	96026	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44397053	74209	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	660	11	4	7	3.8	COC(=O)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL188980	74209	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	660	11	4	7	3.8	COC(=O)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44396957	74734	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	577	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccco3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL191159	74734	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	577	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccco3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		10255546	84106	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	503	8	2	2	5.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCC1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL208367	84106	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	503	8	2	2	5.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCC1CCCCC1	10.1016/j.bmcl.2006.01.016
		156015336	184298	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	3793	77	53	60	-15.9	CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2	10.1021/acs.jmedchem.0c00485
		CHEMBL4639782	184298	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	3793	77	53	60	-15.9	CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2	10.1021/acs.jmedchem.0c00485
		44412729	84212	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	3	7	2.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccco2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208679	84212	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	3	7	2.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccco2)CC1	10.1016/j.bmcl.2006.04.069
		44415764	87893	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c(Cl)cccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215646	87893	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c(Cl)cccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415337	148446	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	619	11	1	3	8.2	CCC(C)[C@H](NCCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL385437	148446	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	619	11	1	3	8.2	CCC(C)[C@H](NCCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44416072	86873	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc3ccccc23)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213153	86873	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc3ccccc23)CC1	10.1016/j.bmcl.2006.06.075
		44416126	87695	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215332	87695	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434781	96679	0	None	-6	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237919	96679	0	None	-6	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434768	161494	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	9	2	2	8.3	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL399811	161494	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	9	2	2	8.3	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		70690147	81858	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	474	10	2	4	2.7	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035945	81858	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	474	10	2	4	2.7	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		70684954	84594	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL2092821	84594	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		44410349	82967	0	None	-	1	Human	4.6	pKi	=	4.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	460	11	2	3	4.8	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccccc1Cl	10.1016/j.bmcl.2006.01.016
		CHEMBL205813	82967	0	None	-	1	Human	4.6	pKi	=	4.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	460	11	2	3	4.8	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccccc1Cl	10.1016/j.bmcl.2006.01.016
		10291369	175701	0	None	-4	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	8	2	2	3.6	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL438672	175701	0	None	-4	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	8	2	2	3.6	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44416122	86903	0	None	1	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL213284	86903	0	None	1	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		44404542	79150	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	323	5	0	4	2.2	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(=O)OC	10.1016/j.bmcl.2005.08.018
		CHEMBL198606	79150	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	323	5	0	4	2.2	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(=O)OC	10.1016/j.bmcl.2005.08.018
		168291110	198799	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5201799	198799	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168271237	197267	0	None	-93	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5179081	197267	0	None	-93	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		46885323	14981	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092209	14981	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44433279	158488	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396433	158488	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11330869	126758	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL349886	126758	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44394079	133543	0	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL365278	133543	0	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44577088	196188	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	6	1	3	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL513128	196188	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	6	1	3	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2008.03.072
		44443029	100472	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	582	9	1	5	6.1	CSc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL247009	100472	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	582	9	1	5	6.1	CSc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44442981	159857	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397608	159857	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11328898	14732	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1090488	14732	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1204059	14732	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		24886498	19062	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184873	19062	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL375388	19062	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		168285465	198411	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5195766	198411	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		24848995	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		CHEMBL340355	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		44391286	129395	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	656	12	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCC2=O)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL360296	129395	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	656	12	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCC2=O)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		24848995	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL340355	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44405561	78716	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	11	2	4	4.6	CC(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197272	78716	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	11	2	4	4.6	CC(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44444452	160872	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	497	9	2	5	3.4	CNCCNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398489	160872	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	497	9	2	5	3.4	CNCCNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		24848995	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL340355	124725	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		44348069	22460	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)cn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL122236	22460	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)cn1C	10.1016/j.bmcl.2004.05.003
		44396954	73619	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	10	3	5	4.0	Cc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL186188	73619	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	10	3	5	4.0	Cc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44434698	177804	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	3	5	8.1	COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL445669	177804	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	3	5	8.1	COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44443043	161439	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	10	0	5	6.2	CC(C)CN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL399570	161439	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	10	0	5	6.2	CC(C)CN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		9968756	96284	0	None	-16	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	5	1	2	3.7	NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237299	96284	0	None	-16	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	5	1	2	3.7	NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		10025669	104167	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL269776	104167	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		11851038	147113	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44401341	142451	0	None	3	2	Human	5.6	pKi	=	5.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	630	13	5	4	4.5	N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL372965	142451	0	None	3	2	Human	5.6	pKi	=	5.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	630	13	5	4	4.5	N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562597	195831	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL509475	195831	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3646886	218803	0	None	29	2	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646886	218803	0	None	29	2	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44447242	101757	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254701	101757	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44432965	152537	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL391665	152537	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432965	152537	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL391665	152537	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44562560	181032	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	463	7	2	4	4.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454905	181032	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	463	7	2	4	4.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL50056	220898	2	None	-7	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44405392	79227	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	2	5	4.8	CC(C)COC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198851	79227	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	2	5	4.8	CC(C)COC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447226	101498	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252993	101498	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44444433	161168	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398756	161168	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447233	161666	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	489	6	1	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400783	161666	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	489	6	1	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447208	162067	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	539	6	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL402917	162067	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	539	6	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		71456251	85810	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	2	5	3.4	CN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113140	85810	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	2	5	3.4	CN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44412770	85277	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	520	9	3	6	1.7	CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211187	85277	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	520	9	3	6	1.7	CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44415369	86379	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2F)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL211462	86379	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2F)CC1	10.1016/j.bmcl.2006.05.088
		44415691	86926	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	585	11	1	3	8.0	CCC(C)CN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		CHEMBL213389	86926	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	585	11	1	3	8.0	CCC(C)CN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		44416020	145890	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL378671	145890	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434760	95292	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	519	9	2	2	7.6	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235140	95292	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	519	9	2	2	7.6	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44443039	161438	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	686	12	0	6	7.3	COc1ccc(CN(Cc2ccc(OC)cc2)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL399564	161438	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	686	12	0	6	7.3	COc1ccc(CN(Cc2ccc(OC)cc2)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		88944284	155305	0	None	-9549	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	986	17	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CCc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3938542	155305	0	None	-9549	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	986	17	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CCc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		11845804	86333	0	None	-616	3	Human	5.5	pKi	=	5.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL211419	86333	0	None	-616	3	Human	5.5	pKi	=	5.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168287469	198300	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5194073	198300	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44562518	193537	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	3	5	3.6	C=CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488884	193537	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	3	5	3.6	C=CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44413876	86519	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		CHEMBL211699	86519	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		168285465	198411	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5195766	198411	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL4211294	220044	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK cell membranes after 1 hr by liquid scintillation counting	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@@H]5CCCN5C1=O)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC3=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N2	10.1021/acs.jmedchem.8b00378
		44434556	151935	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391219	151935	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL438596	220560	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44442998	100381	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL246631	100381	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44443026	161581	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL400263	161581	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44413876	86519	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
		CHEMBL211699	86519	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
		11308054	140394	0	None	8	2	Human	7.5	pKi	=	7.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL371365	140394	0	None	8	2	Human	7.5	pKi	=	7.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562422	185844	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471517	185844	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44395513	72976	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	7	3.9	NCCC(=O)OC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184424	72976	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	7	3.9	NCCC(=O)OC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44396068	134326	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	626	13	4	6	5.0	CC(NCCNc1cccc2ccccc12)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL366303	134326	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	626	13	4	6	5.0	CC(NCCNc1cccc2ccccc12)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44455891	104694	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL272514	104694	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44447229	161727	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	636	10	1	6	5.1	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL401110	161727	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	636	10	1	6	5.1	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		46885367	14624	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089797	14624	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44397216	133610	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	483	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CN)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365491	133610	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	483	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CN)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44416071	86872	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213152	86872	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		1016	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	10519	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		53236833	153346	0	None	-4168	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1024	19	14	11	-1.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3922906	153346	0	None	-4168	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1024	19	14	11	-1.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		168277258	197489	0	None	-5	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5182345	197489	0	None	-5	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL3644285	218708	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644285	218708	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		9842665	163585	12	None	-3	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		88212371	150939	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1039	18	15	12	-2.1	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3904001	150939	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1039	18	15	12	-2.1	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644295	218717	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644361	218773	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590619	132303	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646852	132303	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		117723617	167171	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	16	16	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL4111210	167171	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	16	16	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3644296	218718	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644309	218728	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644323	218742	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644347	218765	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		88590619	132303	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646852	132303	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134137220	149680	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3893727	149680	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		134133748	149948	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3896045	149948	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		134153479	159591	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1134	19	15	12	3.6	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3973826	159591	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1134	19	15	12	3.6	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		90684345	166875	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1040	18	15	11	-2.8	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL4108637	166875	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1040	18	15	11	-2.8	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL3644296	218718	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644323	218742	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644361	218773	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646876	218794	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663317	218828	0	None	-3	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663354	218863	0	None	95	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663357	218866	0	None	1412	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3663379	218887	0	None	17	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667916	218892	0	None	50	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667917	218893	0	None	56	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667922	218897	0	None	63	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667933	218906	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1cccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)c1	nan
		CHEMBL3667941	218914	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944398	159734	0	None	-301	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3975096	159734	0	None	-301	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		1338	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		9938402	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		CHEMBL339053	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		44412574	84830	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209990	84830	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44412612	145703	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	145703	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		44412513	166193	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL410087	166193	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		44400661	131117	0	None	512	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	620	11	2	5	6.1	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL363641	131117	0	None	512	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	620	11	2	5	6.1	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415082	217212	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44577061	199420	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL521715	199420	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		44347840	168703	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		91932630	168703	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL415333	168703	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		24740535	96124	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	544	8	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL236939	96124	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	544	8	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2007.07.097
		23635235	173280	0	None	-1	5	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL427860	173280	0	None	-1	5	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		6918844	175401	1	None	173	4	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF	10.1016/j.bmcl.2005.03.053
		CHEMBL436122	175401	1	None	173	4	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF	10.1016/j.bmcl.2005.03.053
		10369375	83993	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL207946	83993	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		44562460	196044	0	None	165	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL511826	196044	0	None	165	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		1338	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL267492	217503	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432962	152536	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL391664	152536	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432962	152536	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL391664	152536	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434553	96069	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236839	96069	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44434559	96268	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237267	96268	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44577094	185426	0	None	117	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL467588	185426	0	None	117	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44432932	94529	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233758	94529	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432932	94529	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233758	94529	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL2415084	217214	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(N)=O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44577091	185446	0	None	19	3	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467772	185446	0	None	19	3	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		24180592	103788	0	None	5	6	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL266647	103788	0	None	5	6	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		44577060	194831	0	None	1	8	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	194831	0	None	1	8	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44443023	161798	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL401487	161798	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432939	94019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232951	94019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24740653	95367	0	None	190	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		CHEMBL235556	95367	0	None	190	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		44432939	94019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232951	94019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44433284	95345	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	10	2	5	4.2	CC(C)C[C@H](NC(=O)CN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235421	95345	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	10	2	5	4.2	CC(C)C[C@H](NC(=O)CN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433272	154490	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393204	154490	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44432964	94228	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233372	94228	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432964	94228	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233372	94228	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44391405	72859	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	587	10	3	5	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183831	72859	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	587	10	3	5	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		44395615	72939	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	595	13	3	6	4.5	CC(C)CC(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184272	72939	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	595	13	3	6	4.5	CC(C)CC(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644291	218714	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		88590641	131839	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644307	131839	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		117723615	156750	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1066	19	16	12	-1.3	N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3949958	156750	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1066	19	16	12	-1.3	N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3644280	218703	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		88590641	131839	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644307	131839	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644280	218703	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644291	218714	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646864	218786	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3663382	218890	0	None	25	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		166585440	198697	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		CHEMBL5200190	198697	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		44433381	95440	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	626	7	1	4	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235852	95440	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	626	7	1	4	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415707	148307	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	11	2	4	6.3	CCC(C)[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384636	148307	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	11	2	4	6.3	CCC(C)[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447241	161462	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399677	161462	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44443020	100864	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL249065	100864	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL5087814	221898	0	None	-8	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL5087859	221902	0	None	-436	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		10283067	83302	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206042	83302	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL410672	219609	0	None	4	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		168277916	197456	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4986	94	68	63	-6.6	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5181812	197456	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4986	94	68	63	-6.6	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		168284256	197725	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5185775	197725	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432957	93983	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232774	93983	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44415377	87097	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	11	2	5	4.0	CCOCC(NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214204	87097	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	11	2	5	4.0	CCOCC(NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405620	141068	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	2	4	4.2	CC(C)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371703	141068	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	2	4	4.2	CC(C)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		9842665	163585	12	None	-3	2	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44442914	151892	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	4	5.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCC4CCCCC4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL391183	151892	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	4	5.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCC4CCCCC4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46885560	14583	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089485	14583	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44347976	23209	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	404	5	0	3	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL123258	23209	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	404	5	0	3	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C	10.1016/j.bmcl.2004.05.003
		44415748	148260	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cn(C)c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384390	148260	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cn(C)c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44434770	95336	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	521	9	2	2	7.3	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235359	95336	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	521	9	2	2	7.3	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434701	96276	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		CHEMBL237291	96276	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		44434771	155569	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	627	11	3	3	8.6	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL394073	155569	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	627	11	3	3	8.6	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44443010	100778	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	7	1	5	3.9	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248669	100778	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	7	1	5	3.9	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44265751	112875	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL313379	112875	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		44393441	73203	0	None	-2	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL185195	73203	0	None	-2	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL3644286	218709	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644286	218709	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		168278271	197894	0	None	-30	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5187932	197894	0	None	-30	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		11851038	147113	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		11845813	146582	0	None	1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL379879	146582	0	None	1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL5091245	222079	0	None	-7	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137653925	165386	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4092141	165386	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44415966	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL425962	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44400709	175375	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	5	6.4	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1ccccc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL435933	175375	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	5	6.4	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1ccccc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44415966	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL425962	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44562422	185844	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471517	185844	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44433417	155139	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	4.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL393726	155139	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	4.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44416349	87884	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215617	87884	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44415966	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL425962	172880	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44432957	93983	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232774	93983	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		11846669	87052	0	None	1	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		CHEMBL213956	87052	0	None	1	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		24886734	18599	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182130	18599	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL213940	18599	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		44413002	179332	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	11	3	7	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL448475	179332	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	11	3	7	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44442903	152681	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	1	5	4.2	COCC(C)NCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL391780	152681	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	1	5	4.2	COCC(C)NCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347977	175070	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	418	6	0	3	5.8	CCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL434029	175070	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	418	6	0	3	5.8	CCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		44401581	75405	0	None	2	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL191794	75405	0	None	2	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44416109	87683	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	494	8	1	6	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215290	87683	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	494	8	1	6	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmcl.2006.06.075
		44416006	148339	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL384852	148339	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		44434854	96804	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238153	96804	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		11851038	147113	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44443011	160788	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	1	5	4.3	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398408	160788	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	1	5	4.3	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46905544	17071	0	None	-4	2	Human	4.5	pKi	=	4.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	641	14	6	5	2.6	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161791	17071	0	None	-4	2	Human	4.5	pKi	=	4.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	641	14	6	5	2.6	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44265751	112875	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL313379	112875	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL1201469	21279	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		None	nan
		44413535	103480	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL264120	103480	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		44562540	195741	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	582	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CCc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508293	195741	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	582	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CCc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644298	218720	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644298	218720	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44433479	95864	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236526	95864	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		16132144	216058	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44443028	100900	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	9	1	6	5.2	COC(=O)c1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL249270	100900	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	9	1	6	5.2	COC(=O)c1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432913	94157	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233336	94157	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL3577976	218523	0	None	2	2	Mouse	6.5	pKi	=	6.5	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		44444436	101147	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cncn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250797	101147	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cncn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44444443	168551	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	9	0	5	4.2	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL413989	168551	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	9	0	5	4.2	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44348152	23205	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	414	5	0	3	5.2	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL123215	23205	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	414	5	0	3	5.2	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		44348070	120702	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cnc(-c2ccccc2CCc2cc(Br)ccc2OC)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL332584	120702	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cnc(-c2ccccc2CCc2cc(Br)ccc2OC)n1C	10.1016/j.bmcl.2004.05.003
		44562389	182915	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	603	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL459218	182915	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	603	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44434772	95372	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	95372	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434855	96805	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	96805	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434860	96817	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238159	96817	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434757	159520	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	2	4	8.3	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397324	159520	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	2	4	8.3	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434598	96591	0	None	-6	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.5	NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237743	96591	0	None	-6	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.5	NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		88944288	156683	0	None	-12882	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3949338	156683	0	None	-12882	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44412572	145791	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	632	11	2	4	7.2	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378568	145791	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	632	11	2	4	7.2	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		44562421	185843	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	518	9	2	5	3.6	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471516	185843	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	518	9	2	5	3.6	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44391404	129912	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	11	3	5	4.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL361210	129912	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	11	3	5	4.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644290	218713	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O	nan
		117723603	153859	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1072	19	17	12	-3.4	CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3927218	153859	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1072	19	17	12	-3.4	CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644290	218713	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O	nan
		CHEMBL3644341	218760	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3663322	218833	0	None	1	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C#N)c2)NC(=O)[C@H](CCN)NC1=O	nan
		88944296	149373	0	None	-60	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3891338	149373	0	None	-60	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL2415080	217210	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		1338	10579	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		9938402	10579	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		CHEMBL339053	10579	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		44393889	73121	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185094	73121	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44432954	93820	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232585	93820	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432913	94157	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233336	94157	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		168273645	197104	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	5162	106	68	67	-6.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5176443	197104	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	5162	106	68	67	-6.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		168289457	198159	0	None	-20	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5192329	198159	0	None	-20	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432954	93820	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232585	93820	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		168289404	198091	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5191309	198091	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44562363	183750	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	551	12	2	5	5.7	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462379	183750	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	551	12	2	5	5.7	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415085	217215	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		44447231	161686	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400882	161686	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447809	102101	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	480	5	1	4	3.8	CC(=O)N1CC[C@H](c2ccc(F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256540	102101	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	480	5	1	4	3.8	CC(=O)N1CC[C@H](c2ccc(F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442902	152412	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	586	8	1	5	4.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)c4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL391570	152412	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	586	8	1	5	4.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)c4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44415384	148358	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	463	7	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2O)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384965	148358	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	463	7	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2O)CC1	10.1016/j.bmcl.2006.05.088
		44434772	95372	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	95372	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434849	153634	0	None	-17	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	411	9	2	2	5.2	NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		CHEMBL392521	153634	0	None	-17	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	411	9	2	2	5.2	NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		10292084	155174	0	None	-13	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	6	2	2	3.4	NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL393755	155174	0	None	-13	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	6	2	2	3.4	NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		44401513	75937	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	612	13	5	6	2.5	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL192450	75937	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	612	13	5	6	2.5	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		168287469	198300	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5194073	198300	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44391403	72044	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	602	10	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)c2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182823	72044	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	602	10	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)c2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		11157584	175023	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL433710	175023	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		88565601	131841	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644353	131841	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		88565601	131841	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644353	131841	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		11249788	126892	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL351088	126892	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44433483	152542	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL391667	152542	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447765	161853	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NC(=O)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401797	161853	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NC(=O)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44442901	100514	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	600	9	1	5	4.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247230	100514	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	600	9	1	5	4.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10411266	121107	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	5	0	3	6.1	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL333075	121107	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	5	0	3	6.1	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		44397080	73939	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	567	11	3	5	4.2	CC(C)(C)CCNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187657	73939	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	567	11	3	5	4.2	CC(C)(C)CCNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44396955	175004	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	655	10	3	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL433598	175004	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	655	10	3	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44434843	95475	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236020	95475	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	96518	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434684	153377	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	12	2	2	5.0	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL392315	153377	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	12	2	2	5.0	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434845	154681	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	527	10	4	2	6.5	N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393350	154681	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	527	10	4	2	6.5	N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434702	156292	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		CHEMBL394646	156292	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		44443013	100820	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	6	3.3	CS(=O)(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248861	100820	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	6	3.3	CS(=O)(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44412559	162517	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	539	10	2	5	3.0	CCN(CC)CC(C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL405601	162517	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	539	10	2	5	3.0	CCN(CC)CC(C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		46885863	15244	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1093858	15244	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		168290510	198676	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5199932	198676	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5085972	221782	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
		11330992	126712	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349515	126712	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644303	218725	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CSCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646859	218782	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646861	218784	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644303	218725	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CSCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646861	218784	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646866	218788	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663341	218850	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1ccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)cc1OC	nan
		CHEMBL2070254	215964	0	None	7	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44393821	73486	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185583	73486	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		23634985	161608	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23634985	161608	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL400412	161608	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL400412	161608	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		44442978	159855	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397607	159855	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25132867	179277	0	None	6	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
		CHEMBL448337	179277	0	None	6	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
		44412647	85171	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	604	9	2	4	6.5	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(C2CCCCC2)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL211078	85171	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	604	9	2	4	6.5	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(C2CCCCC2)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		168276507	197044	0	None	-87	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5175487	197044	0	None	-87	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44562412	181878	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	602	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL456886	181878	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	602	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44562401	196484	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	570	12	1	4	6.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC2CC2)CC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL515512	196484	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	570	12	1	4	6.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC2CC2)CC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		44322994	113774	0	None	-3	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL315258	113774	0	None	-3	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11341811	126902	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL351161	126902	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		46930943	75180	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		CHEMBL1917059	75180	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44433421	153054	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	568	6	1	4	5.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL392069	153054	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	568	6	1	4	5.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415361	86845	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.05.088
		CHEMBL213041	86845	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.05.088
		46885815	14632	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		CHEMBL1089830	14632	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		44397132	134080	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccccc1C(=O)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365893	134080	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccccc1C(=O)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44434778	96518	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL5092761	222167	0	None	-501	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
		46885907	14812	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL1090885	14812	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		88944400	160070	0	None	-8912	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3977876	160070	0	None	-8912	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44391288	72725	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	608	9	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNc2ccncc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL183610	72725	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	608	9	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNc2ccncc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44433441	96700	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	544	7	1	4	5.9	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(Cc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL237977	96700	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	544	7	1	4	5.9	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(Cc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44397224	74095	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL188432	74095	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44416182	86943	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	511	7	2	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2O)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213469	86943	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	511	7	2	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2O)CC1	10.1016/j.bmcl.2006.06.075
		24741961	96140	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	462	7	1	4	5.0	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236978	96140	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	462	7	1	4	5.0	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		46885712	14843	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1091151	14843	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1204061	14843	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		46885417	15053	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092573	15053	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		25128751	180363	0	None	11	3	Human	7.4	pKi	=	7.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
		CHEMBL453300	180363	0	None	11	3	Human	7.4	pKi	=	7.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
		44397224	74095	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL188432	74095	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44397306	74238	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	576	11	4	6	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3=CC=CCN3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189172	74238	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	576	11	4	6	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3=CC=CCN3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL5080784	221485	0	None	-9	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44412679	85603	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccccc1CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211279	85603	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccccc1CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44415675	86651	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	557	8	1	3	6.5	CCC(C)[C@H](NC(C)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212303	86651	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	557	8	1	3	6.5	CCC(C)[C@H](NC(C)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444446	161655	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	6	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400712	161655	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	6	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44400902	77781	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	3	7	4.0	O=C(N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL195172	77781	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	3	7	4.0	O=C(N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44416045	87187	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	448	7	2	4	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CNc2ccccc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214560	87187	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	448	7	2	4	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CNc2ccccc2)CC1	10.1016/j.bmcl.2006.06.075
		44434884	95386	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235617	95386	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		70682904	84641	0	None	1	2	Human	4.4	pKi	=	4.4	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL2093089	84641	0	None	1	2	Human	4.4	pKi	=	4.4	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		70660687	151688	0	None	-912	2	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	800	16	12	10	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3910197	151688	0	None	-912	2	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	800	16	12	10	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44416014	86790	0	None	16	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL212855	86790	0	None	16	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		88590646	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590646	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590646	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	132308	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44413604	18589	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182065	18589	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL208953	18589	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44409339	81771	0	None	630	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL203252	81771	0	None	630	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL3644302	218724	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	nan
		CHEMBL3644336	218755	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644302	218724	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	nan
		CHEMBL3644336	218755	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL2415086	217216	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		44447238	101695	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CS(=O)(=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254278	101695	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CS(=O)(=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		11398483	94023	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232973	94023	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44442942	100374	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL246605	100374	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11398483	94023	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232973	94023	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44413741	19060	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184861	19060	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL373735	19060	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44391285	71137	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	639	12	3	7	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL181277	71137	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	639	12	3	7	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44455996	162239	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL403924	162239	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		44347330	174842	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL432407	174842	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44455997	104614	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	11	1	6	4.4	COc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272088	104614	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	11	1	6	4.4	COc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		44434880	95385	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235616	95385	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44434685	95946	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	497	14	3	3	6.3	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236638	95946	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	497	14	3	3	6.3	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434691	96200	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	11	2	4	7.0	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL237069	96200	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	11	2	4	7.0	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434695	96201	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	503	9	2	2	7.1	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237070	96201	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	503	9	2	2	7.1	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434855	96805	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	96805	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44401371	77916	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	633	13	5	5	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL195548	77916	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	633	13	5	5	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562324	180185	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.1	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL452838	180185	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.1	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44395654	103348	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.7	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL263066	103348	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.7	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44434579	96208	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	496	8	1	4	4.3	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237080	96208	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	496	8	1	4	4.3	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44447221	101444	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252584	101444	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416161	87183	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214551	87183	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		1338	10579	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44442934	100543	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247422	100543	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11156852	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL183434	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2008.07.076
		44562362	183618	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	505	9	2	4	5.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL461132	183618	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	505	9	2	4	5.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		88878679	154263	0	None	-25118	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1081	19	15	12	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3930415	154263	0	None	-25118	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1081	19	15	12	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		11156852	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL183434	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447237	101694	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254277	101694	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		70681742	81854	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035941	81854	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1	10.1016/j.bmc.2012.04.001
		11156852	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL183434	72459	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		44347082	170687	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL420727	170687	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44395465	73586	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	481	8	1	4	5.4	CC(C)(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL186030	73586	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	481	8	1	4	5.4	CC(C)(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44416093	87087	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	479	8	1	5	4.5	COc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL214155	87087	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	479	8	1	5	4.5	COc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		44434772	95372	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	95372	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434688	95948	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	13	2	2	5.4	NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236640	95948	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	13	2	2	5.4	NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434855	96805	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	96805	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434682	155383	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	451	13	2	2	6.1	NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393919	155383	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	451	13	2	2	6.1	NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434847	95732	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	11	4	2	7.0	N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236442	95732	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	11	4	2	7.0	N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434545	155128	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL393715	155128	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44434545	155128	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL393715	155128	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2007.05.026
		24741964	96152	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236980	96152	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44562367	183707	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	563	8	2	5	5.8	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462010	183707	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	563	8	2	5	5.8	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44393417	103366	0	None	5	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL263182	103366	0	None	5	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44433379	158480	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	622	6	1	5	6.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL396429	158480	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	622	6	1	5	6.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44416338	175659	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL438275	175659	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44442958	161560	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	8	1	6	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccn4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400162	161560	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	8	1	6	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccn4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44395416	129484	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL360422	129484	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415085	217215	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		71450920	85813	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113143	85813	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		51346770	65001	0	None	-3	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
		CHEMBL1682209	65001	0	None	-3	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
		CHEMBL433645	220422	0	None	6	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		89007934	149832	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3895073	149832	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644297	218719	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3646859	218782	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644328	218747	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3644331	218750	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646875	218793	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646881	218799	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646889	218806	0	None	33	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		134142092	153971	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3928099	153971	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3644297	218719	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644331	218750	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644344	218762	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646859	218782	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646875	218793	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646881	218799	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646889	218806	0	None	33	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88287424	135428	0	None	575	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1058	18	17	12	-3.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667919	135428	0	None	575	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1058	18	17	12	-3.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663346	218855	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C(C)(C)C)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663355	218864	0	None	389	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3663362	218871	0	None	107	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663376	218884	0	None	6	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3667920	218895	0	None	39	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667937	218910	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667946	218919	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3667948	218921	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667957	218930	0	None	20	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667960	218933	0	None	58	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		122178168	128039	0	None	25	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577997	128039	0	None	25	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577995	218531	0	None	6	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578000	218533	0	None	50	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		25132866	179390	0	None	77	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
		CHEMBL449131	179390	0	None	77	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
		44569175	195601	0	None	32	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
		CHEMBL506272	195601	0	None	32	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
		44412560	146248	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	593	11	2	5	4.1	CCN(CC)CC(C1CCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379423	146248	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	593	11	2	5	4.1	CCN(CC)CC(C1CCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		44412561	146503	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	11	2	5	4.5	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379823	146503	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	11	2	5	4.5	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		11993702	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		5416	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		9272	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		CHEMBL3301624	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		DB11700	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		44577062	200153	0	None	26	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL525177	200153	0	None	26	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		44432952	93819	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232584	93819	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44562477	193509	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	9	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488710	193509	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	9	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		6918850	132200	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL364560	132200	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44432952	93819	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232584	93819	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		6918850	132200	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL364560	132200	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		42630327	162650	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
		CHEMBL4060381	162650	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
		11993702	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		5416	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		9272	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL3301624	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		DB11700	10365	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL407213	219427	0	None	44	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O	10.1021/jm010165y
		10324857	82767	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205468	82767	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL2331674	216311	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		56851059	75849	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		57390568	75849	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		91930628	75849	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL1923668	75849	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		44444499	161792	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL401466	161792	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432924	94053	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233156	94053	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		44433264	96126	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236940	96126	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400863	75939	0	None	151	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	602	11	2	6	5.8	CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192464	75939	0	None	151	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	602	11	2	6	5.8	CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		166585313	198954	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5204022	198954	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		44434568	95951	0	None	81	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236650	95951	0	None	81	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433264	96126	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236940	96126	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433563	95491	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	584	7	1	4	5.6	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236064	95491	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	584	7	1	4	5.6	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.09.079
		44432924	94053	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233156	94053	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL2370967	216749	0	None	2	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44400932	77078	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	588	11	2	6	5.4	CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194393	77078	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	588	11	2	6	5.4	CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2070242	215962	0	None	1	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44456304	162033	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		CHEMBL402787	162033	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		1338	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44562495	193413	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	561	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488030	193413	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	561	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44444495	161694	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL400932	161694	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44456219	162217	0	None	25	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL403806	162217	0	None	25	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44444495	161694	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL400932	161694	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		11215758	72853	0	None	125	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183799	72853	0	None	125	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		44432909	175748	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL439020	175748	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44444507	100948	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249571	100948	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432909	175748	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL439020	175748	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44433283	103235	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL262320	103235	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44395667	73739	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	12	3	6	4.3	O=C(CC1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186737	73739	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	12	3	6	4.3	O=C(CC1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644333	218752	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		134148066	156752	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1068	18	17	12	2.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](Cc2cnc[nH]2)/N=C\1O	nan
		CHEMBL3949976	156752	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1068	18	17	12	2.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](Cc2cnc[nH]2)/N=C\1O	nan
		CHEMBL3667932	218905	0	None	100	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44447240	101725	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254490	101725	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL267492	217503	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44447806	102325	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	532	6	1	5	3.8	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3S(C)(=O)=O)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL257579	102325	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	532	6	1	5	3.8	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3S(C)(=O)=O)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44404564	133219	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccccc1C(F)(F)F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL365184	133219	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccccc1C(F)(F)F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404561	141636	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	7	0	3	2.2	CCN(CC)CC(Cc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL371896	141636	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	7	0	3	2.2	CCN(CC)CC(Cc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		6918857	145487	1	None	33	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL377961	145487	1	None	33	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.10.103
		44415388	87361	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	12	2	5	5.2	NCCNC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214988	87361	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	12	2	5	5.2	NCCNC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		70688111	81856	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	494	9	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035943	81856	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	494	9	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		44397133	73491	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	671	11	3	6	4.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185625	73491	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	671	11	3	6	4.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415347	148681	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL386868	148681	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416024	86887	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	477	7	1	4	5.1	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL213214	86887	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	477	7	1	4	5.1	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		44434843	95475	0	None	1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236020	95475	0	None	1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		51346771	65000	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
		CHEMBL1682208	65000	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
		CHEMBL438596	220560	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44391315	70681	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	659	14	3	6	5.1	CC(C)COCCCNC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL180545	70681	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	659	14	3	6	5.1	CC(C)COCCCNC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396002	131552	0	None	17	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	587	11	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1	10.1016/j.bmcl.2004.08.055
		CHEMBL364215	131552	0	None	17	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	587	11	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1	10.1016/j.bmcl.2004.08.055
		168279695	197914	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5188196	197914	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44413606	18592	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182088	18592	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211032	18592	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44395535	133164	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	628	12	2	6	4.5	O=C([C@@H](Cc1ccc(Cl)cc1)NS(=O)(=O)CC(F)(F)F)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL365082	133164	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	628	12	2	6	4.5	O=C([C@@H](Cc1ccc(Cl)cc1)NS(=O)(=O)CC(F)(F)F)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44447243	161570	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL400191	161570	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		71452734	85816	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	7	3	5	3.4	CC(=O)NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113146	85816	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	7	3	5	3.4	CC(=O)NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		10077483	84098	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	610	13	2	4	7.1	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)Nc1ccccc1	10.1016/j.bmcl.2006.01.016
		CHEMBL208329	84098	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	610	13	2	4	7.1	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)Nc1ccccc1	10.1016/j.bmcl.2006.01.016
		44415940	87727	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	467	8	1	3	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215354	87727	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	467	8	1	3	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44434704	95947	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236639	95947	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434690	96081	0	None	-4	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	96081	0	None	-4	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434713	96371	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237502	96371	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		11845438	144401	0	None	3	3	Human	6.4	pKi	=	6.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL375775	144401	0	None	3	3	Human	6.4	pKi	=	6.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		25217223	173369	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL428014	173369	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		44562366	183706	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	3	4	4.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)NC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462009	183706	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	3	4	4.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)NC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3646887	218804	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646887	218804	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44405366	78736	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		CHEMBL197327	78736	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		44447823	161822	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401631	161822	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44347378	121212	0	None	5	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	818	11	11	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333262	121212	0	None	5	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	818	11	11	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44400769	134290	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	632	12	2	6	6.4	O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL366171	134290	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	632	12	2	6	6.4	O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44412909	85007	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1C	10.1016/j.bmcl.2006.04.069
		CHEMBL210600	85007	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1C	10.1016/j.bmcl.2006.04.069
		44444437	101183	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250991	101183	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		25217223	173369	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL428014	173369	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		44397223	73891	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	636	10	4	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187439	73891	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	636	10	4	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415941	146939	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL380299	146939	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		24882666	102493	0	None	-1	2	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	385	10	5	3	1.7	N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		CHEMBL258295	102493	0	None	-1	2	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	385	10	5	3	1.7	N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		71461657	85814	0	None	-15	4	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	556	6	2	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113144	85814	0	None	-15	4	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	556	6	2	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		9946241	96207	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.1	NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237079	96207	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.1	NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL3644282	218705	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644282	218705	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644289	218712	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O	nan
		CHEMBL3644330	218749	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644289	218712	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O	nan
		CHEMBL3644330	218749	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44433475	155668	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL394160	155668	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447249	162296	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL404207	162296	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		168285313	198180	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5192562	198180	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168283616	198018	0	None	-20	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5190042	198018	0	None	-20	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44413652	19072	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184921	19072	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL378415	19072	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44396069	73035	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	602	10	2	6	3.9	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(c2ccccc2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184643	73035	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	602	10	2	6	3.9	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(c2ccccc2)CC1	10.1016/j.bmcl.2004.08.055
		44443005	101297	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251698	101297	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44415790	86865	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1OC	10.1016/j.bmcl.2006.05.088
		CHEMBL213125	86865	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1OC	10.1016/j.bmcl.2006.05.088
		44434699	96275	0	None	-1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	531	10	2	3	7.7	CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237290	96275	0	None	-1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	531	10	2	3	7.7	CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44413968	87004	0	None	-229	3	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL213751	87004	0	None	-229	3	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		11296732	150591	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL390130	150591	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44435184	154970	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	476	7	1	4	5.3	Cc1ccc([C@H](N)CC(C)C)c(N2CCN(C(=O)C(C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL393583	154970	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	476	7	1	4	5.3	Cc1ccc([C@H](N)CC(C)C)c(N2CCN(C(=O)C(C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		11296732	150591	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL390130	150591	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44443021	100896	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249267	100896	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		168295173	199090	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5206293	199090	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168270124	196734	0	None	-33	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5170533	196734	0	None	-33	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432960	94075	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233175	94075	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44322924	113889	0	None	-3	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL316038	113889	0	None	-3	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44412685	86515	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)OCc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211680	86515	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)OCc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		44416092	86581	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	463	7	1	4	4.8	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL212024	86581	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	463	7	1	4	4.8	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		44434778	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434709	96550	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	563	9	2	2	7.7	NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237714	96550	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	563	9	2	2	7.7	NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434863	154923	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393552	154923	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434665	154727	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393383	154727	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265347	103742	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	10	4	4	3.3	NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL266305	103742	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	10	4	4	3.3	NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44413592	85192	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL211131	85192	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL3644320	218739	0	None	75	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646874	218792	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644320	218739	0	None	75	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646874	218792	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663328	218839	0	None	-1	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C#N)NC(=O)[C@H](CCN)NC1=O	nan
		52919529	159398	0	None	-4466	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1038	19	14	11	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3972160	159398	0	None	-4466	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1038	19	14	11	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88944180	159457	0	None	-2951	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	987	20	14	11	-1.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3972716	159457	0	None	-2951	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	987	20	14	11	-1.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		168279695	197914	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5188196	197914	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432960	94075	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233175	94075	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		25217225	159068	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL396940	159068	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44447807	175513	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	6	1	5	3.7	COc1ccc([C@H]2CCN(C(C)=O)[C@H]2C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)cc1	10.1016/j.bmcl.2008.01.125
		CHEMBL437032	175513	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	6	1	5	3.7	COc1ccc([C@H]2CCN(C(C)=O)[C@H]2C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)cc1	10.1016/j.bmcl.2008.01.125
		44397124	130461	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	641	11	3	5	5.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL362158	130461	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	641	11	3	5	5.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168272660	197212	0	None	-57	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5178164	197212	0	None	-57	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		25217225	159068	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL396940	159068	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44412678	145447	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377762	145447	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44444468	161437	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	567	10	1	5	4.4	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(=O)CCN	10.1016/j.bmcl.2007.06.088
		CHEMBL399557	161437	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	567	10	1	5	4.4	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(=O)CCN	10.1016/j.bmcl.2007.06.088
		44416023	86886	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213213	86886	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434700	156288	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	637	12	3	4	9.0	CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL394645	156288	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	637	12	3	4	9.0	CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		88878636	159630	0	None	-114	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	944	17	13	10	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3974162	159630	0	None	-114	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	944	17	13	10	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		168285904	198449	0	None	-9	3	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5196407	198449	0	None	-9	3	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44562458	185798	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.2	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471166	185798	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.2	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44395466	73735	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.6	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3CNCCc3cccs3)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186732	73735	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.6	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3CNCCc3cccs3)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644319	218738	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644319	218738	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		44413932	144324	0	None	1	3	Human	7.3	pKi	=	7.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
		CHEMBL375440	144324	0	None	1	3	Human	7.3	pKi	=	7.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
		44413687	19063	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184874	19063	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL375389	19063	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL443590	220704	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		11353522	63956	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164884	63956	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44415725	84724	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	453	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccs2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209601	84724	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	453	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccs2)CC1	10.1016/j.bmcl.2006.05.088
		44416108	87611	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	465	7	2	5	4.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(O)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215238	87611	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	465	7	2	5	4.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(O)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44443012	100779	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	8	2	5	4.1	CCNC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248670	100779	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	8	2	5	4.1	CCNC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404540	79168	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	279	4	1	3	1.3	CC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198665	79168	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	279	4	1	3	1.3	CC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44562519	201324	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CCC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL529449	201324	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CCC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44391379	70255	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.9	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL179889	70255	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.9	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644313	218732	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@](C)(Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644313	218732	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@](C)(Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434552	96068	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c([C@H](N)CC(C)C)cccc2C(F)(F)F)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236838	96068	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c([C@H](N)CC(C)C)cccc2C(F)(F)F)CC1	10.1016/j.bmc.2007.05.026
		44444490	101281	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	7	1	4	5.3	CC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL251587	101281	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	7	1	4	5.3	CC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		44444508	161861	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL401853	161861	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44415965	86687	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212451	86687	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44401553	76600	0	None	18	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	648	14	4	5	3.7	COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1	10.1016/j.bmcl.2005.03.120
		CHEMBL193715	76600	0	None	18	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	648	14	4	5	3.7	COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1	10.1016/j.bmcl.2005.03.120
		44396067	73006	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	548	10	4	6	3.8	CC(Nc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184542	73006	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	548	10	4	6	3.8	CC(Nc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44455956	161815	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	10	1	5	4.7	Cc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL401593	161815	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	10	1	5	4.7	Cc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		88944290	155978	0	None	-4677	2	Human	5.3	pKi	=	5.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3943941	155978	0	None	-4677	2	Human	5.3	pKi	=	5.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434778	96518	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434655	96797	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	12	2	2	5.6	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238135	96797	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	12	2	2	5.6	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44404538	79138	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	315	5	1	4	0.7	CN1CCN(C(CNS(C)(=O)=O)c2ccccc2F)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198544	79138	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	315	5	1	4	0.7	CN1CCN(C(CNS(C)(=O)=O)c2ccccc2F)CC1	10.1016/j.bmcl.2005.08.018
		46905545	17072	0	None	2	2	Human	5.3	pKi	=	5.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	631	14	7	6	1.4	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161792	17072	0	None	2	2	Human	5.3	pKi	=	5.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	631	14	7	6	1.4	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		137658158	166496	0	None	-16	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4104465	166496	0	None	-16	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44395899	176099	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL441675	176099	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3663344	218853	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(N)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667935	218908	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168285313	198180	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5192562	198180	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		46885711	14842	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
		CHEMBL1091150	14842	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
		44447248	101477	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252825	101477	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412910	145151	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(C)(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377186	145151	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(C)(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL2370966	216748	0	None	-39	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44444427	161188	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	436	4	0	4	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C#N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL398854	161188	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	436	4	0	4	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C#N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416074	146316	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	468	8	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCNC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL379591	146316	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	468	8	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCNC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44435220	96027	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	10	2	3	8.9	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236803	96027	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	10	2	3	8.9	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434715	174287	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	593	10	2	3	7.8	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		CHEMBL429983	174287	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	593	10	2	3	7.8	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		71458056	85805	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	541	6	3	4	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3cc[nH]c23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113135	85805	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	541	6	3	4	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3cc[nH]c23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44404577	78728	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	295	4	1	4	1.5	COC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197289	78728	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	295	4	1	4	1.5	COC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		2683	109665	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL305906	109665	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL334255	109665	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		44433273	96445	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	4.9	CNCCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237577	96445	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	4.9	CNCCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44562598	181040	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	9	3	5	4.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCCNC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454917	181040	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	9	3	5	4.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCCNC2)CC1	10.1016/j.bmcl.2008.07.076
		44323031	174857	0	None	-8	3	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL432565	174857	0	None	-8	3	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391402	130430	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2cccnc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL361985	130430	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2cccnc2)CC1	10.1016/j.bmcl.2004.10.096
		168295173	199090	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5206293	199090	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44393851	129867	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360989	129867	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44434554	96178	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237049	96178	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		71452721	85748	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	580	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3nccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2113035	85748	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	580	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3nccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415521	148213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL384138	148213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		44393876	129345	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360169	129345	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44415521	148213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384138	148213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444438	161634	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cccn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400595	161634	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cccn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44397054	132569	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	9	3	5	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C(F)(F)F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL364772	132569	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	9	3	5	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C(F)(F)F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415746	86612	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(S(C)(=O)=O)cc2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212146	86612	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(S(C)(=O)=O)cc2)CC1	10.1016/j.bmcl.2006.05.088
		44434713	96371	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237502	96371	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434584	158721	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	394	6	1	3	4.9	NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL396638	158721	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	394	6	1	3	4.9	NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		11845630	146292	0	None	5	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL379490	146292	0	None	5	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		44433295	95859	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236520	95859	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400812	78075	0	None	457	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	667	12	3	5	6.3	O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195734	78075	0	None	457	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	667	12	3	5	6.3	O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400778	142666	0	None	162	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	574	10	2	6	5.0	COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL373099	142666	0	None	162	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	574	10	2	6	5.0	COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44409338	175523	0	None	1230	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL437132	175523	0	None	1230	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		44415918	148327	0	None	-2	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL384774	148327	0	None	-2	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44323029	213960	0	None	-1	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL92481	213960	0	None	-1	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL3644279	218702	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644329	218748	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](N)CN2C1=O	nan
		CHEMBL3646880	218798	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646885	218802	0	None	47	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646892	218809	0	None	51	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		134134506	150454	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3900116	150454	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3644279	218702	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646880	218798	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646885	218802	0	None	47	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646892	218809	0	None	51	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663359	218868	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663380	218888	0	None	8	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663382	218890	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667921	218896	0	None	81	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667934	218907	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667936	218909	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667955	218928	0	None	20	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667962	218935	0	None	107	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		122178169	128040	0	None	31	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577998	128040	0	None	31	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577999	218532	0	None	19	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44413668	146294	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	621	13	2	5	5.4	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL379497	146294	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	621	13	2	5	5.4	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2006.04.016
		1338	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44432930	174260	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL429943	174260	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44569176	179324	0	None	19	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
		CHEMBL448410	179324	0	None	19	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
		25133209	180130	0	None	53	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
		CHEMBL452710	180130	0	None	53	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
		44412574	84830	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209990	84830	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44412642	145460	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	13	2	5	5.6	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377825	145460	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	13	2	5	5.6	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44432930	174260	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL429943	174260	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44410188	147158	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
		CHEMBL380854	147158	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
		44432948	157010	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395227	157010	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		25133556	195628	0	None	3	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
		CHEMBL506762	195628	0	None	3	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
		44432948	157010	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395227	157010	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL428326	220217	0	None	-10	4	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
		44416152	87873	0	None	38	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215576	87873	0	None	38	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44456027	162249	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL403967	162249	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
		44456259	174045	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	566	7	0	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL429314	174045	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	566	7	0	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.10.115
		44577059	200106	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	536	9	2	4	4.7	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL524443	200106	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	536	9	2	4	4.7	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		10304794	146183	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	146183	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44433446	158743	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396660	158743	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44577063	194879	0	None	70	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL498150	194879	0	None	70	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44577060	194831	0	None	-1	8	Rat	8.3	pKi	=	8.3	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	194831	0	None	-1	8	Rat	8.3	pKi	=	8.3	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		23661656	175823	0	None	1	5	Mouse	8.3	pKi	=	8.3	Binding	Binding affinity to C57BL/6J mouse MC4 receptorBinding affinity to C57BL/6J mouse MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	175823	0	None	1	5	Mouse	8.3	pKi	=	8.3	Binding	Binding affinity to C57BL/6J mouse MC4 receptorBinding affinity to C57BL/6J mouse MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44442997	100697	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248205	100697	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		25129453	178545	0	None	14	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
		CHEMBL446757	178545	0	None	14	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
		CHEMBL2370964	216746	0	None	-7	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44322795	213705	0	None	13	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL91041	213705	0	None	13	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		16007263	86571	0	None	41	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL211975	86571	0	None	41	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		23635236	98376	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635236	98376	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240780	98376	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240780	98376	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
		44432956	155362	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL393903	155362	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		10283036	147021	0	None	72	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	647	11	2	5	5.2	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380540	147021	0	None	72	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	647	11	2	5	5.2	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1	10.1016/j.bmcl.2005.10.103
		44432956	155362	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL393903	155362	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		23635237	98228	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635237	98228	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
		CHEMBL240364	98228	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240364	98228	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
		44416286	145690	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	455	7	1	3	5.5	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL378327	145690	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	455	7	1	3	5.5	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		44395869	74010	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	579	11	3	6	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL187957	74010	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	579	11	3	6	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3646888	218805	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646888	218805	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44432917	179501	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL450577	179501	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		46885481	14527	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089104	14527	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44404547	142572	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL373042	142572	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71454510	85824	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113154	85824	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		168287698	198576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198280	198576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5077144	221264	0	None	-32	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44432917	179501	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL450577	179501	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44562440	185820	0	None	27	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471340	185820	0	None	27	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		71450919	85806	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.3	CC(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113136	85806	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.3	CC(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434663	95290	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	483	13	3	3	5.9	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235138	95290	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	483	13	3	3	5.9	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434778	96518	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		10109225	161451	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	3	3.2	NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL399624	161451	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	3	3.2	NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690145	81844	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	420	8	3	4	1.6	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CNC[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035931	81844	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	420	8	3	4	1.6	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CNC[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		44265496	103824	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL267020	103824	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL3644288	218711	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644288	218711	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	nan
		44455893	162417	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL404706	162417	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44432902	154405	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL393134	154405	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		44432902	154405	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL393134	154405	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		88944368	150280	0	None	-2630	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3898758	150280	0	None	-2630	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44444449	160868	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	1	4	4.9	CC(C)CNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398488	160868	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	1	4	4.9	CC(C)CNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44442900	100513	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247229	100513	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44391386	138226	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	616	11	4	6	3.7	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL369104	138226	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	616	11	4	6	3.7	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		11157584	175023	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL433710	175023	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447820	102286	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.1	CCCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257374	102286	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.1	CCCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447773	102481	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL258245	102481	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443025	100898	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	6	5.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc([N+](=O)[O-])cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249269	100898	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	6	5.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc([N+](=O)[O-])cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46885523	14575	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		CHEMBL1089461	14575	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		44412964	84143	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	522	11	4	7	1.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCO)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208553	84143	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	522	11	4	7	1.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCO)CC1	10.1016/j.bmcl.2006.04.069
		44444425	100915	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	5	0	4	4.1	COc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249348	100915	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	5	0	4	4.1	COc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44444454	100921	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNC3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249376	100921	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNC3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44396956	131157	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	643	10	3	5	4.9	CC(C)(C)c1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL363877	131157	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	643	10	3	5	4.9	CC(C)(C)c1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44434690	96081	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	96081	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44562391	196624	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	504	9	2	4	5.3	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL516659	196624	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	504	9	2	4	5.3	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		71456243	85737	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	8	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113020	85737	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	8	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44394078	168496	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL413556	168496	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44447781	162043	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402822	162043	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		168293467	198930	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5203840	198930	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		11262020	127045	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352457	127045	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		71459941	85817	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.2	CN(C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1)S(C)(=O)=O	10.1016/j.bmcl.2005.07.035
		CHEMBL2113147	85817	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.2	CN(C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1)S(C)(=O)=O	10.1016/j.bmcl.2005.07.035
		44434867	95298	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235162	95298	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44434769	96514	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	659	11	3	3	9.6	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237698	96514	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	659	11	3	3	9.6	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		70694364	81850	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	304	5	4	5	-1.1	NCCNC(=O)[C@@H]1CNC[C@H]1C(=O)NC(=O)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035937	81850	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	304	5	4	5	-1.1	NCCNC(=O)[C@@H]1CNC[C@H]1C(=O)NC(=O)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL3644284	218707	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644284	218707	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88944367	155069	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3936714	155069	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44562520	198518	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	568	10	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)Cc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL519729	198518	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	568	10	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)Cc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		137637711	162625	0	None	-20	3	Mouse	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting method	ChEMBL	871	11	14	12	-3.9	C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O	10.1021/acs.jmedchem.7b00856
		CHEMBL4060087	162625	0	None	-20	3	Mouse	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting method	ChEMBL	871	11	14	12	-3.9	C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O	10.1021/acs.jmedchem.7b00856
		168287698	198576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198280	198576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44447810	161812	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	5	1	4	4.7	CC(=O)N1CC[C@H](c2ccc(C(F)(F)F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401584	161812	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	5	1	4	4.7	CC(=O)N1CC[C@H](c2ccc(C(F)(F)F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44412665	84645	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	578	10	2	4	5.9	CC(C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209325	84645	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	578	10	2	4	5.9	CC(C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44443035	161196	0	None	-26	4	Human	6.3	pKi	=	6.3	Binding	Binding affinity to MC5RBinding affinity to MC5R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	161196	0	None	-26	4	Human	6.3	pKi	=	6.3	Binding	Binding affinity to MC5RBinding affinity to MC5R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		53236832	158692	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1002	19	13	12	-0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3966176	158692	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1002	19	13	12	-0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44433420	95445	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	542	5	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235893	95445	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	542	5	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44397226	168442	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	647	11	4	7	3.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL413064	168442	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	647	11	4	7	3.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44395534	73535	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.5	NC(CC(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL185852	73535	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.5	NC(CC(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44434633	95945	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	423	11	2	2	5.3	NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236630	95945	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	423	11	2	2	5.3	NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265496	103824	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL267020	103824	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168293467	198930	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5203840	198930	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		44393850	72871	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL183890	72871	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447821	174241	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C3CCC3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL429853	174241	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C3CCC3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44412681	144973	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccc(CC(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL376973	144973	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccc(CC(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		44444444	168668	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	494	6	0	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL415086	168668	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	494	6	0	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447764	102317	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	552	7	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2(Cc3ccc(Cl)cc3)COC(=O)N2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257538	102317	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	552	7	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2(Cc3ccc(Cl)cc3)COC(=O)N2)CC1	10.1016/j.bmcl.2008.01.125
		44434772	95372	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	95372	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		70688108	81846	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	418	8	4	4	1.7	O=C(CNC(=O)[C@H]1CNC[C@H]1C(=O)NCCc1c[nH]c2ccccc12)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035933	81846	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	418	8	4	4	1.7	O=C(CNC(=O)[C@H]1CNC[C@H]1C(=O)NCCc1c[nH]c2ccccc12)c1ccccc1	10.1016/j.bmc.2012.04.001
		70683847	81847	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	390	7	4	3	2.0	O=C(NCCc1c[nH]c2ccccc12)[C@@H]1CNC[C@@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035934	81847	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	390	7	4	3	2.0	O=C(NCCc1c[nH]c2ccccc12)[C@@H]1CNC[C@@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		25133903	177337	0	None	7	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
		CHEMBL445009	177337	0	None	7	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
		5624	39467	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL1203324	39467	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL141343	39467	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		44413881	144371	0	None	-1	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL375559	144371	0	None	-1	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		44433275	158486	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	647	14	1	5	6.0	CCN(CC)CCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396432	158486	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	647	14	1	5	6.0	CCN(CC)CCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44391391	71412	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccn2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL181788	71412	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccn2)CC1	10.1016/j.bmcl.2004.10.096
		44415630	86806	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	4	5.9	CCC(C)[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212897	86806	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	4	5.9	CCC(C)[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447772	102438	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)C3NCCC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL258036	102438	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)C3NCCC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		46885524	14576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1089462	14576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1204054	14576	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		44562594	180934	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	503	9	1	4	5.5	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454670	180934	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	503	9	1	4	5.5	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44455957	161849	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	10	1	5	4.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL401792	161849	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	10	1	5	4.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44412691	145170	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	12	4	7	3.1	COc1ccccc1CNC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377269	145170	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	12	4	7	3.1	COc1ccccc1CNC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		9842665	163585	12	None	-3	2	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44447771	161992	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	5	2	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402587	161992	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	5	2	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44442956	101123	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL250701	101123	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44434759	95291	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235139	95291	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434690	96081	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	96081	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434714	155171	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393753	155171	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44265591	178822	0	None	-1	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	499	12	7	4	2.3	N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(02)00089-6
		CHEMBL447178	178822	0	None	-1	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	499	12	7	4	2.3	N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(02)00089-6
		44265487	104158	0	None	-2	4	Human	4.3	pKi	=	4.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	256	6	4	2	1.8	N=C(N)NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL269689	104158	0	None	-2	4	Human	4.3	pKi	=	4.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	256	6	4	2	1.8	N=C(N)NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44433292	159572	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	10	2	5	5.0	CC(C)C[C@H](NC(=O)C(C)(C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397368	159572	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	10	2	5	5.0	CC(C)C[C@H](NC(=O)C(C)(C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44323020	175775	0	None	-7	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	951	11	12	9	1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL439188	175775	0	None	-7	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	951	11	12	9	1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		10077594	82365	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		CHEMBL204670	82365	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		168290484	198633	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	5	1	7	3.9	Cc1nc2c(cc1-c1cnn(C)c1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5199107	198633	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	5	1	7	3.9	Cc1nc2c(cc1-c1cnn(C)c1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		44415359	146324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	511	8	1	4	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL379625	146324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	511	8	1	4	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		11845450	145247	0	None	-44	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377465	145247	0	None	-44	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		11238126	172127	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL423619	172127	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44400770	140327	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	598	12	3	7	5.0	O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL370926	140327	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	598	12	3	7	5.0	O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44415926	148160	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	453	7	1	3	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL383849	148160	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	453	7	1	3	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44434872	95339	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235382	95339	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44393430	131141	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	524	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL363757	131141	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	524	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL3646878	218796	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646878	218796	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		44413577	146304	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379531	146304	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		44347106	121838	0	None	46	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	738	9	10	7	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL334309	121838	0	None	46	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	738	9	10	7	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44323233	113493	0	None	4	2	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL314401	113493	0	None	4	2	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		11364326	73460	0	None	-27	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		CHEMBL185455	73460	0	None	-27	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		44433450	95260	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	502	7	2	5	3.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCO)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234984	95260	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	502	7	2	5	3.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCO)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44444435	161624	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cnnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400510	161624	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cnnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44562284	195818	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	601	16	0	4	8.2	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL509340	195818	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	601	16	0	4	8.2	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44434572	173371	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	9	2	2	4.6	NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL428022	173371	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	9	2	2	4.6	NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690146	81845	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	433	8	3	3	2.9	O=C(NCc1ccc(C(F)(F)F)cc1)[C@@H]1CNC[C@@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035932	81845	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	433	8	3	3	2.9	O=C(NCc1ccc(C(F)(F)F)cc1)[C@@H]1CNC[C@@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL5075506	221158	0	None	-457	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44433391	161710	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.6	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL401025	161710	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.6	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL438596	220560	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44447822	102326	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257584	102326	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44413938	145717	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL378446	145717	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		9958649	131135	0	None	-53	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
		CHEMBL363730	131135	0	None	-53	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
		44447244	101322	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL251814	101322	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44415727	148559	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	10	1	3	8.2	CCC(C)[C@H](NCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL386123	148559	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	10	1	3	8.2	CCC(C)[C@H](NCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434666	95334	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	434	9	1	3	5.8	NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235356	95334	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	434	9	1	3	5.8	NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	96518	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	96518	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434654	96796	0	None	-21	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.4	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238134	96796	0	None	-21	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.4	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44433286	176030	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.4	CNCC(=O)N[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL441136	176030	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.4	CNCC(=O)N[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416060	88093	0	None	52	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215895	88093	0	None	52	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88565595	131843	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644355	131843	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644345	218763	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644351	218769	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644358	218771	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](N)CN2C1=O	nan
		CHEMBL3646882	218800	0	None	19	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646891	218808	0	None	25	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88565595	131843	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644355	131843	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		134134990	150684	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3901972	150684	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3644345	218763	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644351	218769	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3646882	218800	0	None	19	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646891	218808	0	None	25	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663352	218861	0	None	63	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL3663358	218867	0	None	69	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](C(C)C)NC1=O	nan
		CHEMBL3663381	218889	0	None	15	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667929	218902	0	None	43	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667956	218929	0	None	23	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		10030530	24371	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL125819	24371	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL2415083	217213	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44434558	96267	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237266	96267	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		23635106	98332	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635106	98332	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240568	98332	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240568	98332	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		24740312	96147	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236979	96147	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		25129105	183798	0	None	23	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
		CHEMBL463047	183798	0	None	23	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
		25129109	195481	0	None	16	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
		CHEMBL504349	195481	0	None	16	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
		44412513	166193	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL410087	166193	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		44433265	152854	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	576	10	1	4	5.7	CCN[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391915	152854	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	576	10	1	4	5.7	CCN[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		6918847	183751	1	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	526	9	2	6	2.6	CCOC(=O)[C@H]1CCCC[C@@H]1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462380	183751	1	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	526	9	2	6	2.6	CCOC(=O)[C@H]1CCCC[C@@H]1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		11490658	71717	0	None	301	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182277	71717	0	None	301	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		122178162	128034	0	None	-	1	Mouse	8.2	pKi	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577991	128034	0	None	-	1	Mouse	8.2	pKi	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433267	96239	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	592	11	2	5	4.7	CC(C)C[C@H](NCCO)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237147	96239	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	592	11	2	5	4.7	CC(C)C[C@H](NCCO)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433262	152851	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391914	152851	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11296600	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL360716	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		11296600	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360716	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44433262	152851	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391914	152851	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		10283067	83302	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206042	83302	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		11296600	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL360716	129721	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		44397198	73539	0	None	93	3	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells; Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells;	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185862	73539	0	None	93	3	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells; Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells;	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44432933	93568	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232164	93568	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44416197	172757	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL425261	172757	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44432933	93568	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232164	93568	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447804	162373	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404503	162373	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44433426	175803	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	6.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCCCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL439387	175803	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	6.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCCCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL264132	217385	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cncn2C)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		16038315	145536	0	None	309	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	13	3	7	3.5	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378046	145536	0	None	309	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	13	3	7	3.5	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		1338	10579	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		24886259	18598	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182116	18598	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL213340	18598	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		168271899	197380	0	None	3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3020	70	35	39	-5.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5180727	197380	0	None	3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3020	70	35	39	-5.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433269	96313	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237364	96313	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11226756	126752	0	None	23	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349850	126752	0	None	23	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644322	218741	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644322	218741	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		44405395	142040	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	10	2	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cccnc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL372576	142040	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	10	2	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cccnc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416160	88099	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	513	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215905	88099	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	513	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		44432898	93801	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232532	93801	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44397280	74077	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	13	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL188341	74077	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	13	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168286369	198491	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2962	64	33	37	-4.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197030	198491	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2962	64	33	37	-4.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432898	93801	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232532	93801	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44347379	121213	0	None	4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	750	9	9	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333263	121213	0	None	4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	750	9	9	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44395436	73633	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186239	73633	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415017	217207	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmc.2013.06.052
		9852314	85807	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113137	85807	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434690	96081	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	96081	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434821	96803	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	441	10	4	2	4.5	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238149	96803	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	441	10	4	2	4.5	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44455958	161850	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL401793	161850	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2007.10.115
		44405382	139606	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	651	10	2	5	5.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cnc4ccccc4c3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL370178	139606	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	651	10	2	5	5.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cnc4ccccc4c3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44397121	130205	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361719	130205	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168271934	196864	0	None	-34	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5172738	196864	0	None	-34	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
		44433564	103234	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	632	7	1	4	7.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL262319	103234	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	632	7	1	4	7.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44415809	88266	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	10	1	6	5.1	COc1cc(OC)c(OC)cc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL216009	88266	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	10	1	6	5.1	COc1cc(OC)c(OC)cc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		137638725	163758	0	None	-1	2	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4073016	163758	0	None	-1	2	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		137659790	166101	0	None	-5	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL4099889	166101	0	None	-5	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137636965	162995	0	None	-5	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4064433	162995	0	None	-5	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL438030	220523	0	None	-1	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44447819	162199	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.7	CCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403699	162199	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.7	CCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443016	100863	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL249064	100863	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		46885415	15051	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092571	15051	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44397225	174997	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	645	11	4	6	4.1	CN(C)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL433555	174997	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	645	11	4	6	4.1	CN(C)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44415442	145702	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	11	1	4	6.6	COCCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL378397	145702	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	11	1	4	6.6	COCCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44348151	120745	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	428	5	0	3	5.6	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL332602	120745	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	428	5	0	3	5.6	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		10134057	95432	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	8	2	3	3.6	C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235815	95432	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	8	2	3	3.6	C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434636	96075	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	469	12	3	3	5.6	NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236841	96075	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	469	12	3	3	5.6	NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690148	81859	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	464	10	3	5	1.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCO)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035946	81859	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	464	10	3	5	1.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCO)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		10158674	154693	0	None	-8	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.4	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393359	154693	0	None	-8	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.4	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		25131477	185480	0	None	27	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
		CHEMBL468252	185480	0	None	27	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
		88944403	154055	0	None	-6309	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	979	16	13	10	-0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3928766	154055	0	None	-6309	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	979	16	13	10	-0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		122178165	128037	0	None	-	1	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577994	128037	0	None	-	1	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577978	218525	0	None	10	2	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		10260053	174982	0	None	-4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433413	174982	0	None	-4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		11237928	171650	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL422027	171650	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44432897	154403	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393133	154403	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		10053261	147324	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	548	12	2	4	5.2	CCN(CC)CCCC(C)/N=C(/NC)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL381085	147324	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	548	12	2	4	5.2	CCN(CC)CCCC(C)/N=C(/NC)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		137646617	164323	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4080223	164323	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44413913	145451	0	None	1	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL377779	145451	0	None	1	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		11756904	83361	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
		CHEMBL206316	83361	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
		88590620	131840	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644352	131840	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88590620	131840	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644352	131840	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667931	218904	0	None	154	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44433424	153341	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	8	1	5	4.7	COCC(C)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL392287	153341	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	8	1	5	4.7	COCC(C)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44415692	87099	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214217	87099	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		46885558	14581	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089483	14581	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL5094168	222258	0	None	-436	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11387898	62822	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL162493	62822	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		11353851	64246	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL165746	64246	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		88944280	151862	0	None	-213	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	922	15	13	10	-1.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3911582	151862	0	None	-213	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	922	15	13	10	-1.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		44415747	148259	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	486	7	2	3	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c[nH]c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384389	148259	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	486	7	2	3	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c[nH]c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44432897	154403	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393133	154403	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44395503	73730	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	496	10	2	5	4.2	NCC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186696	73730	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	496	10	2	5	4.2	NCC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44434662	95289	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.6	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235137	95289	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.6	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434754	97011	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238345	97011	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434601	153246	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	8	1	2	4.3	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL392223	153246	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	8	1	2	4.3	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		9969456	154395	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	7	2	2	4.7	NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393125	154395	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	7	2	2	4.7	NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265711	213768	0	None	-4	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	343	6	3	2	3.5	NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL9138	213768	0	None	-4	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	343	6	3	2	3.5	NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		1338	10579	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	10579	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	10579	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL3667952	218925	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(=O)O)NC1=O	nan
		CHEMBL3667951	218924	0	None	15	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(=O)O)NC1=O	nan
		44401275	75809	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	647	12	5	5	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(C(=O)c2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL192354	75809	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	647	12	5	5	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(C(=O)c2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562289	195738	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508284	195738	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		44433411	173740	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	614	10	1	4	6.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL428731	173740	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	614	10	1	4	6.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44443027	161799	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL401488	161799	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11341045	72940	0	None	-36	4	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
		CHEMBL184275	72940	0	None	-36	4	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
		44434868	156330	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	635	11	5	4	6.7	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL394669	156330	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	635	11	5	4	6.7	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44562538	181155	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1ccccc1CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL455188	181155	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1ccccc1CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562539	181157	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1cccc(CC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)c1	10.1016/j.bmcl.2008.07.076
		CHEMBL455189	181157	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1cccc(CC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)c1	10.1016/j.bmcl.2008.07.076
		44395647	129884	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	11	3	6	3.8	CC(C)(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL361074	129884	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	11	3	6	3.8	CC(C)(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644334	218753	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		134144957	157462	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1059	19	17	12	2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCC(N)=O)/N=C\1O	nan
		CHEMBL3955830	157462	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1059	19	17	12	2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCC(N)=O)/N=C\1O	nan
		44394010	132203	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL364577	132203	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433380	95262	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL234992	95262	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL91957	222684	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11375529	126929	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL351400	126929	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		70688109	81851	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	399	6	3	3	3.4	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)Nc1cccc(-c2ccccc2)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035938	81851	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	399	6	3	3	3.4	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)Nc1cccc(-c2ccccc2)c1	10.1016/j.bmc.2012.04.001
		44265658	16952	0	None	-14	2	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	314	8	4	3	1.4	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)O	10.1016/s0960-894x(02)00089-6
		CHEMBL1159698	16952	0	None	-14	2	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	314	8	4	3	1.4	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)O	10.1016/s0960-894x(02)00089-6
		10132207	95426	0	None	-18	3	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	343	5	2	2	3.9	NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235797	95426	0	None	-18	3	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	343	5	2	2	3.9	NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44413970	145793	0	None	-14	3	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL378571	145793	0	None	-14	3	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		44401418	130794	0	None	2	2	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	621	14	6	4	3.3	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL362964	130794	0	None	2	2	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	621	14	6	4	3.3	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44433388	95347	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
		CHEMBL235432	95347	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
		44416200	88100	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215906	88100	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		44416162	148367	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL385003	148367	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		168283984	198025	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2937	64	35	39	-7.9	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190172	198025	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2937	64	35	39	-7.9	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44322869	112937	0	None	-6	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313690	112937	0	None	-6	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44413537	146325	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379627	146325	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		70688110	81853	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035940	81853	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		44443007	160618	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	4.5	CC(C)C(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398266	160618	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	4.5	CC(C)C(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44413831	84839	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL210008	84839	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		44347990	22498	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	6	0	3	6.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C(C)C	10.1016/j.bmcl.2004.05.003
		CHEMBL122253	22498	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	6	0	3	6.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C(C)C	10.1016/j.bmcl.2004.05.003
		44453902	102209	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	391	10	5	3	2.4	N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		CHEMBL257040	102209	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	391	10	5	3	2.4	N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		10155513	158320	0	None	-7	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	2	4.0	C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396303	158320	0	None	-7	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	2	4.0	C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44322895	170149	0	None	-11	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL419307	170149	0	None	-11	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44433392	95348	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.0	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235433	95348	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.0	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447824	162283	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404141	162283	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44413666	18595	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182095	18595	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211475	18595	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		88878645	152597	0	None	-22387	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1053	19	15	12	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3917089	152597	0	None	-22387	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1053	19	15	12	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44265639	16951	0	None	-5	4	Human	5.2	pKi	=	5.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL1159697	16951	0	None	-5	4	Human	5.2	pKi	=	5.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		44434690	96680	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237920	96680	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		10178845	96689	0	None	-6	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	8	2	3	3.8	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237937	96689	0	None	-6	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	8	2	3	3.8	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265479	212868	0	None	1	2	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	268	2	2	2	1.9	N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1	10.1016/s0960-894x(02)00088-4
		CHEMBL8561	212868	0	None	1	2	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	268	2	2	2	1.9	N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1	10.1016/s0960-894x(02)00088-4
		23635105	161758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635105	161758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL401250	161758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL401250	161758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		11468019	73758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL186841	73758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44413602	18591	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182085	18591	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL210922	18591	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44410385	146632	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
		CHEMBL379918	146632	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
		44415429	86802	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	467	8	1	4	4.5	CCOCC(N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212889	86802	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	467	8	1	4	4.5	CCOCC(N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44442989	100661	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	9	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248028	100661	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	9	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44348039	23196	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cn(C)c(-c2ccccc2CCc2cc(Br)ccc2OC)n1	10.1016/j.bmcl.2004.05.003
		CHEMBL123149	23196	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cn(C)c(-c2ccccc2CCc2cc(Br)ccc2OC)n1	10.1016/j.bmcl.2004.05.003
		137646333	164701	0	None	-4	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4084386	164701	0	None	-4	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44433289	158491	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396434	158491	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44415912	146004	0	None	10	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL378837	146004	0	None	10	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL3644317	218736	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644326	218745	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646879	218797	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644317	218736	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644326	218745	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646879	218797	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3663350	218859	0	None	18	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663374	218882	0	None	8	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667926	218899	0	None	245	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667930	218903	0	None	34	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667950	218923	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667958	218931	0	None	36	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667961	218934	0	None	53	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		136024005	94076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233176	94076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44412758	172818	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	641	10	1	6	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)n2cc3ccccc3c2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL425609	172818	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	641	10	1	6	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)n2cc3ccccc3c2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		136024005	94076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233176	94076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434560	96269	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237268	96269	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44444493	161909	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL402058	161909	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		44456410	104214	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL270015	104214	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44447779	101818	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL255099	101818	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44432928	174422	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL430165	174422	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44322896	174751	0	None	1	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL431801	174751	0	None	1	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44456138	102128	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL256686	102128	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		10232787	147159	0	None	165	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380855	147159	0	None	165	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44432928	174422	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL430165	174422	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447804	162373	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404503	162373	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44434557	152227	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391427	152227	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44455922	161915	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL402075	161915	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
		44577060	194831	0	None	-2	8	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	194831	0	None	-2	8	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44432947	93771	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232387	93771	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432947	93771	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232387	93771	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44456336	162877	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		CHEMBL406309	162877	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		44397028	130809	0	None	61	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1	10.1016/j.bmcl.2005.05.017
		CHEMBL363019	130809	0	None	61	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1	10.1016/j.bmcl.2005.05.017
		44562478	200882	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	9	3	5	4.2	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL528108	200882	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	9	3	5	4.2	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44444504	161696	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL400934	161696	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL2070373	215965	0	None	14	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44433266	96238	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	604	11	0	4	6.4	CCN(CC)[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237146	96238	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	604	11	0	4	6.4	CCN(CC)[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10098971	130802	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL362985	130802	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmcl.2005.03.053
		44432906	155677	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL394167	155677	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL5076315	221207	0	None	1	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44432906	155677	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL394167	155677	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		11468019	73758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186841	73758	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		60168008	81857	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	528	9	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		CHEMBL2035944	81857	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	528	9	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		44404568	79073	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	309	6	0	3	3.0	CCN(CC)CC(c1ccccc1Cl)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198320	79073	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	309	6	0	3	3.0	CCN(CC)CC(c1ccccc1Cl)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404570	79091	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	6	0	3	2.6	CCN(CC)CC(c1ccccc1C)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198378	79091	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	6	0	3	2.6	CCN(CC)CC(c1ccccc1C)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		58777892	85819	0	None	4	4	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113149	85819	0	None	4	4	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		24886735	86506	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	579	10	2	5	3.9	CCN(CC)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCC1	10.1016/j.bmcl.2006.04.002
		CHEMBL211616	86506	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	579	10	2	5	3.9	CCN(CC)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCC1	10.1016/j.bmcl.2006.04.002
		44410207	168538	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
		CHEMBL413931	168538	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
		14364677	77406	2	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	204	2	0	2	2.0	CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL195009	77406	2	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	204	2	0	2	2.0	CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71452733	85812	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113142	85812	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		44434759	95291	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235139	95291	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434603	96688	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	409	10	2	2	4.9	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237935	96688	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	409	10	2	2	4.9	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10292876	154732	0	None	-1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	7	2	2	3.8	NCCCN(C(=O)CCc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL393387	154732	0	None	-1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	7	2	2	3.8	NCCCN(C(=O)CCc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		71461662	85891	0	None	-6	4	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	442	9	4	3	3.2	NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL2113280	85891	0	None	-6	4	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	442	9	4	3	3.2	NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00088-4
		137640703	163876	0	None	-54	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4074479	163876	0	None	-54	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44447227	161667	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400786	161667	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416194	87387	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		CHEMBL215106	87387	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		44412963	84142	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	4	7	2.0	CCC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208552	84142	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	4	7	2.0	CCC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44413056	86656	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	597	10	4	6	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212325	86656	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	597	10	4	6	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL438596	220560	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		156010247	183851	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	2913	40	44	46	-16.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.0c00485
		CHEMBL4633001	183851	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	2913	40	44	46	-16.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.0c00485
		44434634	96074	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	1	5	6.5	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL236840	96074	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	1	5	6.5	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		44434651	96675	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	495	13	3	3	6.1	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237911	96675	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	495	13	3	3	6.1	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		25132525	183504	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
		CHEMBL460142	183504	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
		168296741	199050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5205686	199050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5094215	222260	0	None	-6	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11295737	126991	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352063	126991	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44432916	94332	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233544	94332	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		10211466	175679	0	None	19	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.1	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL438432	175679	0	None	19	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.1	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		1334	8283	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		16133814	8283	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		CHEMBL437050	8283	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		44432916	94332	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233544	94332	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44434851	96684	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	10	2	2	5.7	NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237930	96684	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	10	2	2	5.7	NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434864	97024	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238369	97024	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1	10.1016/j.bmc.2007.06.003
		88878672	160378	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	952	21	14	12	-3.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3980632	160378	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	952	21	14	12	-3.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44415406	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL213738	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44415406	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL213738	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44415406	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL213738	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		44433561	152290	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL391481	152290	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44415406	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213738	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447234	101693	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254276	101693	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447802	102523	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	6	1	5	4.8	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(F)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL258412	102523	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	6	1	5	4.8	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(F)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		10291370	152744	0	None	-8	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	7	2	2	4.1	C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391823	152744	0	None	-8	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	7	2	2	4.1	C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434787	155571	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	729	13	3	5	9.1	COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL394075	155571	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	729	13	3	5	9.1	COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434687	166271	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	465	14	2	2	6.5	NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL410179	166271	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	465	14	2	2	6.5	NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10269187	96891	0	None	-15	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.5	NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL238180	96891	0	None	-15	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.5	NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		137631599	163305	0	None	-109	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4067967	163305	0	None	-109	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		70660693	158568	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	894	17	13	11	-3.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3965058	158568	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	894	17	13	11	-3.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44396036	175122	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL434345	175122	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3663324	218835	0	None	-5	2	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		168296741	199050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5205686	199050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433407	158989	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	586	8	1	4	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396866	158989	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	586	8	1	4	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44415405	86988	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC[C@H](C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213691	86988	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC[C@H](C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415406	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL213738	87001	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44442941	159504	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397312	159504	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		24886501	18596	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182101	18596	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211792	18596	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		44405526	79184	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198723	79184	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44412990	84224	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	4	7	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208694	84224	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	4	7	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44443041	161684	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	0	5	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN(C)Cc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400870	161684	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	0	5	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN(C)Cc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		168272615	197166	0	None	-6	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5177494	197166	0	None	-6	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44409206	146962	0	None	-1	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL380437	146962	0	None	-1	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		44442977	100589	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247636	100589	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133907	183503	0	None	9	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		CHEMBL460138	183503	0	None	9	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		44413880	84721	0	None	-50	3	Human	6.1	pKi	=	6.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
		CHEMBL209587	84721	0	None	-50	3	Human	6.1	pKi	=	6.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
		11308184	71673	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL182231	71673	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44432958	93984	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232775	93984	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		10049407	84105	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
		CHEMBL208366	84105	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
		44433158	161711	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	463	11	2	6	5.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL401027	161711	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	463	11	2	6	5.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44434848	95743	0	None	-5	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		CHEMBL236443	95743	0	None	-5	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		44434854	96804	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238153	96804	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		71458055	85803	0	None	-15	4	Human	5.1	pKi	=	5.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.7	CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL2113133	85803	0	None	-15	4	Human	5.1	pKi	=	5.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.7	CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44434637	96187	0	None	-9	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.3	NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237052	96187	0	None	-9	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.3	NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		71454495	85740	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113023	85740	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL3667949	218922	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		44433406	174121	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)C4CCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL429445	174121	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)C4CCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44432958	93984	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232775	93984	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44447812	102139	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256746	102139	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44415706	87922	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	599	10	1	4	7.1	CCC(C)[C@H](NCC1CCCO1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215741	87922	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	599	10	1	4	7.1	CCC(C)[C@H](NCC1CCCO1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44456460	104251	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)cc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL270202	104251	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)cc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44434785	155570	0	None	-3	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	623	11	2	4	7.8	COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL394074	155570	0	None	-3	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	623	11	2	4	7.8	COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434561	96363	0	None	-1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	433	13	1	2	6.6	CCCCCN(Cc1ccc(N(CC)CC)cc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237478	96363	0	None	-1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	433	13	1	2	6.6	CCCCCN(Cc1ccc(N(CC)CC)cc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44405361	141815	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		CHEMBL371945	141815	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		44447817	102285	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL257373	102285	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		46885480	14526	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089103	14526	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44447239	160585	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.2	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL398236	160585	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.2	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL3644318	218737	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646853	218776	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3646863	218785	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644346	218764	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646890	218807	0	None	37	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		134149606	155317	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3938651	155317	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3644318	218737	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644346	218764	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646863	218785	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646890	218807	0	None	37	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88287941	135430	0	None	23	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667924	135430	0	None	23	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3639667	218698	0	None	64	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663347	218856	0	None	38	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663365	218873	0	None	-1	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3667959	218932	0	None	11	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		25128749	185249	0	None	25	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
		CHEMBL466380	185249	0	None	25	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
		44412612	145703	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	145703	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		25058412	196219	0	None	120	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL513404	196219	0	None	120	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44416299	87333	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	471	8	1	4	5.2	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214886	87333	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	471	8	1	4	5.2	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		168275776	197088	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5176092	197088	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5087839	221899	0	None	-11	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		16172929	219780	15	None	-9	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		CHEMBL412536	219780	15	None	-9	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		44562440	185820	0	None	27	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471340	185820	0	None	27	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44432945	93571	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232186	93571	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44443034	161480	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	8	1	6	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc5c(c4)OCO5)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399766	161480	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	8	1	6	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc5c(c4)OCO5)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44432945	93571	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232186	93571	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44397030	74143	0	None	57	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	607	11	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL188651	74143	0	None	57	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	607	11	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		1338	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44433439	96699	0	None	44	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL237976	96699	0	None	44	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		16132144	216058	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44433268	159010	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	642	11	2	5	5.6	CC(C)C[C@H](NCCO)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396884	159010	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	642	11	2	5	5.6	CC(C)C[C@H](NCCO)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180493	161903	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL402043	161903	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432946	93770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232386	93770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434575	96084	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236872	96084	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44412898	84430	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	549	12	3	6	2.8	COCC(C)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208860	84430	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	549	12	3	6	2.8	COCC(C)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44416183	86619	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	475	7	1	3	5.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL212180	86619	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	475	7	1	3	5.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		44432946	93770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232386	93770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44397198	73539	0	None	93	3	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185862	73539	0	None	93	3	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44444502	161695	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL400933	161695	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		10414731	83323	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL206141	83323	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
		1338	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		9938402	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL339053	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL3644314	218733	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3644314	218733	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CN)NC1=O	nan
		44405376	78778	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	620	11	2	5	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3cccs3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197435	78778	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	620	11	2	5	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3cccs3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416184	86773	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	427	7	1	3	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212779	86773	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	427	7	1	3	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		71458059	85825	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113155	85825	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434754	97011	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238345	97011	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44401392	75432	0	None	-1	2	Human	5.1	pKi	=	5.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	582	14	5	4	3.1	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL191975	75432	0	None	-1	2	Human	5.1	pKi	=	5.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	582	14	5	4	3.1	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL2221249	216222	0	None	-4	3	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O	nan
		44394081	73000	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL184526	73000	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433478	174290	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	472	5	1	4	4.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL429985	174290	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	472	5	1	4	4.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		1338	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	10579	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		168281389	197701	0	None	-22	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5185405	197701	0	None	-22	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
		168284733	198403	0	None	-24	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5195641	198403	0	None	-24	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44447207	101316	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251784	101316	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447207	101316	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL251784	101316	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL2415018	217208	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44434650	96674	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	11	2	2	4.8	NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237910	96674	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	11	2	2	4.8	NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434600	155381	0	None	-7	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	9	2	2	4.0	NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393918	155381	0	None	-7	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	9	2	2	4.0	NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44413842	145155	0	None	-5	3	Human	5.1	pKi	=	5.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377210	145155	0	None	-5	3	Human	5.1	pKi	=	5.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168279040	197961	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	481	3	1	5	5.3	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(Cl)cc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5189093	197961	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	481	3	1	5	5.3	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(Cl)cc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		44433378	96963	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CNC[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL238208	96963	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CNC[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405425	78635	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		CHEMBL197020	78635	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		44415902	146806	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL380018	146806	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44562392	177135	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	645	12	1	6	6.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL444749	177135	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	645	12	1	6	6.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		44577054	194395	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	431	6	1	3	4.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL494818	194395	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	431	6	1	3	4.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL438596	220560	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44434781	96679	0	None	-6	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237919	96679	0	None	-6	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		137660993	166226	0	None	-213	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4101216	166226	0	None	-213	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44393820	73452	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185427	73452	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44405402	78738	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	2	4	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccccc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197329	78738	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	2	4	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccccc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		11249545	72978	0	None	-141	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1	10.1021/jm0400496
		CHEMBL184432	72978	0	None	-141	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1	10.1021/jm0400496
		11375764	73463	0	None	-398	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		CHEMBL185469	73463	0	None	-398	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		44444447	100837	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	0	5	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCN(C)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL248963	100837	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	0	5	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCN(C)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44434861	97022	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238367	97022	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434649	152590	0	None	-3	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	12	2	2	6.4	NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391705	152590	0	None	-3	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	12	2	2	6.4	NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		46885816	14678	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1090161	14678	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		44456416	174021	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	555	10	1	6	4.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccoc2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL429252	174021	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	555	10	1	6	4.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccoc2)CC1	10.1016/j.bmcl.2007.10.115
		44432918	159295	1	None	-	1	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	591	14	2	7	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCNC(=O)OC(C)(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL397140	159295	1	None	-	1	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	591	14	2	7	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCNC(=O)OC(C)(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44396120	73710	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	540	9	2	6	2.4	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(C)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186629	73710	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	540	9	2	6	2.4	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(C)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644327	218746	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644327	218746	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44415346	88090	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215886	88090	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.05.088
		44392514	130645	0	None	2	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL362670	130645	0	None	2	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		88944347	149964	0	None	-13182	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3896173	149964	0	None	-13182	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44323234	174835	0	None	-7	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL432377	174835	0	None	-7	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44322812	119159	0	None	-2	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL329586	119159	0	None	-2	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391316	130718	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	658	11	3	7	3.4	CC(NCCN1CCOCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL362841	130718	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	658	11	3	7	3.4	CC(NCCN1CCOCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644279	218702	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644279	218702	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44444511	100784	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248687	100784	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447235	101724	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254487	101724	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412896	146241	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	3	7	2.2	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379417	146241	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	3	7	2.2	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44562496	193511	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	478	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CO)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488716	193511	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	478	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CO)CC1	10.1016/j.bmcl.2008.07.076
		9842665	163585	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44434664	95333	0	None	-2	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235355	95333	0	None	-2	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL3644280	218703	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644280	218703	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644359	218772	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)NC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644359	218772	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		44265473	213135	1	None	9	2	Human	5.1	pKi	=	5.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	200	4	2	2	1.9	NCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8743	213135	1	None	9	2	Human	5.1	pKi	=	5.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	200	4	2	2	1.9	NCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		10050686	82791	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		CHEMBL205553	82791	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		44562364	183765	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	10	2	5	5.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462559	183765	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	10	2	5	5.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		71450911	85736	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	N[C@H]1CCCC[C@@H]1NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113019	85736	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	N[C@H]1CCCC[C@@H]1NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44415659	84824	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	2	4	6.3	CCC(C)[C@H](NC[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209954	84824	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	2	4	6.3	CCC(C)[C@H](NC[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		168279267	197779	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186603	197779	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		88944179	157831	0	None	-1380	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	16	13	10	-1.3	CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3958741	157831	0	None	-1380	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	16	13	10	-1.3	CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		9842665	163585	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	163585	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		11851038	147113	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	147113	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		24740310	96028	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236804	96028	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44265351	212544	0	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	8	2	3	4.7	N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL8287	212544	0	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	8	2	3	4.7	N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168277543	197454	0	None	-8	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5181752	197454	0	None	-8	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44562561	181033	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454906	181033	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644350	218768	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3646865	218787	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88227239	160199	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	18	17	12	-3.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3979009	160199	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	18	17	12	-3.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644338	218757	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644357	218770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC[S+](C)[O-])NC1=O	nan
		CHEMBL3644338	218757	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644350	218768	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644357	218770	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC[S+](C)[O-])NC1=O	nan
		CHEMBL3646865	218787	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646871	218789	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663377	218885	0	None	3	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3667918	218894	0	None	38	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168275776	197088	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5176092	197088	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		1324	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	7090	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		25129107	180556	0	None	19	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
		CHEMBL453734	180556	0	None	19	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
		1338	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		9938402	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		CHEMBL339053	10579	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		23661656	175823	0	None	-1	5	Rat	8.0	pKi	=	8.0	Binding	Binding affinity to rat MC4 receptorBinding affinity to rat MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	175823	0	None	-1	5	Rat	8.0	pKi	=	8.0	Binding	Binding affinity to rat MC4 receptorBinding affinity to rat MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44416327	87376	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.6	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215066	87376	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.6	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44433481	155669	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	4	5.8	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL394161	155669	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	4	5.8	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		16132144	216058	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	216058	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	216058	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	216058	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44562287	181027	0	None	102	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454900	181027	0	None	102	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL409636	219552	0	None	-1	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm030119t
		25211670	181039	0	None	56	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454916	181039	0	None	56	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		24741625	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236731	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24741625	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236731	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		23634986	98213	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23634986	98213	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL240357	98213	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240357	98213	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		44432951	93567	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232163	93567	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		24741625	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL236731	95967	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		44432951	93567	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232163	93567	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		1338	10579	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	10579	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	10579	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		44394009	131128	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363684	131128	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44456368	102299	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL257447	102299	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL438596	220560	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44443022	161578	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400249	161578	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11846673	86769	0	None	3	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL212766	86769	0	None	3	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44404560	179331	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL448473	179331	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		10075878	82766	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205461	82766	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		70685980	81848	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	337	6	3	3	1.5	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035935	81848	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	337	6	3	3	1.5	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		44404822	77073	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	3.1	CS(=O)(=O)N1CCCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL194368	77073	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	3.1	CS(=O)(=O)N1CCCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44404823	132177	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	621	7	2	6	2.8	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL364553	132177	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	621	7	2	6	2.8	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44562438	185714	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	560	10	2	5	4.6	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL470301	185714	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	560	10	2	5	4.6	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		168279267	197779	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186603	197779	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168294114	198969	0	None	-40	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4756	82	66	59	-5.7	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5204285	198969	0	None	-40	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4756	82	66	59	-5.7	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5078687	221359	0	None	-6	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44415767	87060	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		CHEMBL214000	87060	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		44444448	100838	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL248964	100838	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416251	148659	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL386707	148659	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		44447818	102185	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL256956	102185	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44397122	73629	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	598	11	3	6	3.9	N#Cc1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL186227	73629	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	598	11	3	6	3.9	N#Cc1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		10072440	82790	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	8	2	3	4.2	CCCC/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205552	82790	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	8	2	3	4.2	CCCC/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		44415985	87859	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215519	87859	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434782	96802	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	511	10	2	2	7.5	NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238144	96802	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	511	10	2	2	7.5	NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434856	161171	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	535	14	2	4	5.0	NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL398777	161171	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	535	14	2	4	5.0	NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		88944401	153028	0	None	-9332	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	16	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3920516	153028	0	None	-9332	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	16	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		168282596	197685	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2990	66	33	37	-3.8	CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5185132	197685	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2990	66	33	37	-3.8	CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.2c00786
		44348046	23284	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	4	1	3	5.0	Cn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1O	10.1016/j.bmcl.2004.05.003
		CHEMBL123660	23284	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	4	1	3	5.0	Cn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1O	10.1016/j.bmcl.2004.05.003
		44400834	134172	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	516	9	2	5	4.6	N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL365940	134172	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	516	9	2	5	4.6	N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44433482	176225	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2CN(Cc3ccccc3)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL442703	176225	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2CN(Cc3ccccc3)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415418	86922	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213381	86922	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447801	175556	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	5	4.7	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL437406	175556	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	5	4.7	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44434648	154938	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.1	NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393558	154938	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.1	NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265309	212441	1	None	-2	3	Human	4.0	pKi	=	4.0	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	214	5	2	2	2.3	NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8201	212441	1	None	-2	3	Human	4.0	pKi	=	4.0	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	214	5	2	2	2.3	NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL3644304	218726	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644304	218726	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	nan
		88944292	157377	0	None	-2398	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1001	21	14	11	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3955172	157377	0	None	-2398	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1001	21	14	11	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		44433383	95305	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	7	1	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(S(C)(=O)=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235214	95305	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	7	1	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(S(C)(=O)=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		10304463	83549	0	None	9	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	615	11	1	5	5.6	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206840	83549	0	None	9	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	615	11	1	5	5.6	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.10.103
		44444445	161625	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	0	4	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400511	161625	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	0	4	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		71452731	85808	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.5	CC(C)S(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113138	85808	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.5	CC(C)S(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44433382	95263	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	2	5	4.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)CN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234993	95263	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	2	5	4.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)CN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447768	102386	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	488	6	2	4	4.8	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257827	102386	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	488	6	2	4	4.8	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44347110	120886	0	None	5	3	Human	6.0	pKi	=	6.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	681	9	9	7	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL332762	120886	0	None	5	3	Human	6.0	pKi	=	6.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	681	9	9	7	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44434841	95476	0	None	-30	3	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	455	11	4	2	4.9	N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236022	95476	0	None	-30	3	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	455	11	4	2	4.9	N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434659	154724	0	None	-2	2	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	384	11	2	5	2.6	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc([N+](=O)[O-])cc1	10.1016/j.bmc.2007.06.003
		CHEMBL393382	154724	0	None	-2	2	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	384	11	2	5	2.6	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc([N+](=O)[O-])cc1	10.1016/j.bmc.2007.06.003
		44405403	147129	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	618	10	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccc(F)cc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL380768	147129	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	618	10	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccc(F)cc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447808	102099	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	476	5	1	4	4.0	CC(=O)N1CC[C@H](c2ccc(C)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256539	102099	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	476	5	1	4	4.0	CC(=O)N1CC[C@H](c2ccc(C)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		46885759	15048	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
		CHEMBL1092548	15048	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
		44413828	146071	0	None	5	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL379168	146071	0	None	5	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		44322986	112874	0	None	-2	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL313377	112874	0	None	-2	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		88878683	150630	0	None	-1949	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	973	19	14	11	-2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3901634	150630	0	None	-1949	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	973	19	14	11	-2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88944297	160929	0	None	-218	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	21	15	11	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3985463	160929	0	None	-218	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	21	15	11	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		44433484	95969	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236737	95969	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447767	162418	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL404710	162418	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		25128748	196770	0	None	28	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
		CHEMBL517108	196770	0	None	28	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
		44434686	153378	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	407	11	3	3	4.7	CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		CHEMBL392316	153378	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	407	11	3	3	4.7	CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		44434595	155651	0	None	-1	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	419	9	2	3	5.6	CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL394149	155651	0	None	-1	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	419	9	2	3	5.6	CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL1923663	215865	0	None	-549	3	Human	6.0	pKi	=	6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		44562476	192794	0	None	-	1	Human	7.0	pKi	=	7	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487044	192794	0	None	-	1	Human	7.0	pKi	=	7	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44405362	175062	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL433991	175062	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		46885760	15050	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
		CHEMBL1092550	15050	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
		46930943	75180	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		CHEMBL1917059	75180	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44265672	16953	0	None	-4	4	Human	5.0	pKi	=	5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	442	10	5	3	3.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL1159699	16953	0	None	-4	4	Human	5.0	pKi	=	5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	442	10	5	3	3.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00089-6
		44434656	96798	0	None	-37	3	Human	4.0	pKi	=	4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	401	10	2	2	5.2	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238136	96798	0	None	-37	3	Human	4.0	pKi	=	4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	401	10	2	2	5.2	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10408	7507	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		5329	7507	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		9941379	7507	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		CHEMBL2070241	7507	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		DB11653	7507	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		11993702	10365	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		5416	10365	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		9272	10365	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		CHEMBL3301624	10365	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		DB11700	10365	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		1321	8723	0	None	15	3	Human	8.5	pKd	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10051117
		1340	9250	0	None	-	1	Human	10.1	pKd	None	10.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	546	11	0	5	5.7	COc1ccc2c(c1CCCCN1CCN(CC1)C[C@H](c1ccc(cc1)F)N1CCN(CC1)C(C)C)cccc2	12538838
		6918688	9250	0	None	-	1	Human	10.1	pKd	None	10.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	546	11	0	5	5.7	COc1ccc2c(c1CCCCN1CCN(CC1)C[C@H](c1ccc(cc1)F)N1CCN(CC1)C(C)C)cccc2	12538838
		1329	7102	0	None	-19	3	Mouse	7.3	pKd	None	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9454589
		1328	8724	0	None	10	4	Human	9.5	pKd	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9832440
		7046	223227	0	125I-NDP-MSH	-	1	Human	8.0	pKi	=	8.0	Binding	NoneNone	PDSP KiDatabase	133	0	1	1	1.3	C1CNCC2=CC=CC=C21	None
		None	223089	0	125I-[Nle4,D-Phe7]Alpha-MSH	-93	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	961	29	13	12	-1.5	CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N	None
		None	224375	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	376	4	0	2	4.9	C1CCC(CC1)C(=O)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	224376	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	391	4	1	2	4.8	C1CCC(CC1)NC(=O)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	224377	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	365	6	1	2	4.3	CCCCNC(=O)N1CCCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3	None
		None	224378	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	407	4	1	2	5.0	C1CCC(CC1)NC(=S)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	223088	0	125I-NDP-MSH	-70	4	Human	7.7	pKi	=	7.7	Binding	NoneNone	PDSP KiDatabase	299	5	3	6	-0.3	CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O	None
		None	223088	0	125I-[Nle4,D-Phe7]Alpha-MSH	-70	4	Human	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	299	5	3	6	-0.3	CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O	None
		1016	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2561	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2733526	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		5384	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		CHEMBL83	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		DB00675	10519	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2726	7706	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		621	7706	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		83	7706	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL71	7706	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB00477	7706	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		2247	7293	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		249	7293	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		2603	7293	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		CHEMBL296419	7293	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		DB00637	7293	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		176	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2157	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2566	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		CHEMBL633	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		DB01118	7186	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		4189	213701	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL1559	213701	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL91	213701	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		134611880	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		16132265	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		3633	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		4931	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		CHEMBL1201610	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		DB01285	7066	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		131839615	219415	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		16133835	219415	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		CHEMBL407070	219415	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		10408	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		10408	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		5329	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		5329	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		9941379	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		9941379	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		CHEMBL2070241	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		CHEMBL2070241	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		DB11653	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		DB11653	7507	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		134611880	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		16132265	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		3633	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		4931	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		CHEMBL1201610	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		DB01285	7066	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		1321	8723	0	None	15	3	Human	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9630346
		11993702	10365	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		5416	10365	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		9272	10365	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		CHEMBL3301624	10365	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		DB11700	10365	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		11993702	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		11993702	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		5416	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		5416	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		9272	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		9272	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		CHEMBL3301624	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		CHEMBL3301624	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		DB11700	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		DB11700	10365	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		1320	7154	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1320	7154	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16162729	7154	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16162729	7154	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1323	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1323	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1323	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		92432	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		92432	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		92432	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		CHEMBL430239	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL430239	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		CHEMBL430239	9465	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		1324	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1324	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1324	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		16154396	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16154396	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16154396	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		16197727	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16197727	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16197727	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		44285019	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		44285019	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		44285019	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		57514683	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		57514683	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		57514683	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		91898441	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		91898441	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		91898441	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		CHEMBL441738	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL441738	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		CHEMBL441738	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		DB04931	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		DB04931	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		DB04931	7090	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		1325	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1325	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		6440621	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		6440621	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		9898183	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		9898183	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		CHEMBL3422426	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL3422426	10372	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491

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